Therapeutic agents useful for treating pain

ABSTRACT

A compound of formula: 
                         
wherein Ar 1 , A, R 3 , x, and m are as disclosed herein and Ar 2  is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson&#39;s disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington&#39;s chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Benzoazolylpiperazine Compound are disclosed.

This application claims the benefit of U.S. Provisional Application No.60/435,917, filed Dec. 24, 2002; U.S. Provisional Application No.60/459,626, filed Apr. 3, 2003; and U.S. Provisional Application No.60/473,856, filed May 29, 2003, all of which are incorporated herein byreference in their entirety.

1. FIELD OF THE INVENTION

The present invention relates to Benzoazolylpiperazine Compounds,compositions comprising a Benzoazolylpiperazine Compound and methods fortreating or preventing pain, urinary incontinence (UI), an ulcer,inflammatory-bowel disease (IBD), irritable-bowel syndrome (IBS), anaddictive disorder, Parkinson's disease, parkinsonism, anxiety,epilepsy, stroke, a seizure, a pruritic condition, psychosis, acognitive disorder, a memory deficit, restricted brain function,Huntington's chorea, amyotrophic lateral sclerosis (ALS), dementia,retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia ordepression, comprising administering to an animal in need thereof aneffective amount of a Benzoazolylpiperazine Compound.

2. BACKGROUND OF THE INVENTION

Pain is the most common symptom for which patients seek medical adviceand treatment. Pain can be acute or chronic. While acute pain is usuallyself-limited, chronic pain persists for 3 months or longer and can leadto significant changes in a patient's personality, lifestyle, functionalability and overall quality of life (K. M. Foley, Pain, in CecilTextbook of Medicine 100-107(J. C. Bennett and F. Plum eds., 20th ed.1996)).

Pain has been traditionally managed by administering non-opioidanalgesics, such as acetylsalicylic acid, choline magnesiumtrisalicylate, acetaminophen, ibuprofen, fenoprofen, diflusinal, andnaproxen; or opioid analgesics, including morphine, hydromorphone,methadone, levorphanol, fentanyl, oxycodone, and oxymorphone. Id.

UI is uncontrollable urination, generally caused bybladder-detrusor-muscle instability. UI affects people of all ages andlevels of physical health, both in health care settings and in thecommunity at large. At present, UI afflicts 15-30% of elderly peopleliving at home, one-third of those living in acute-care settings, and atleast one-half of those living in long-term care institutions (R. M.Resnick, Lancet 346:94 (1995)). Persons having UI are predisposed toalso having urinary-tract infections, pressure ulcers, perineal rashesand urosepsis. Psychosocially, UI is associated with embarrassment,social stigmatization, depression and a risk of institutionalization(Herzo et al., Annu. Rev. Gerontol. Geriatr. 9:74 (1989)). Economically,the costs of UI are great; in the United States alone, health-care costsassociated with UI are over $15 billion per annum.

Physiologic bladder contraction results in large part fromacetylcholine-induced stimulation of post-ganglionic muscarinic-receptorsites on bladder smooth muscle. Treatments for UI include theadministration of drugs having bladder-relaxant properties, which helpto control bladder-detrusor-muscle overactivity. For example,anticholinergics such as propantheline bromide and glycopyrrolate, andcombinations of smooth-muscle relaxants such as a combination of racemicoxybutynin and dicyclomine or an anticholinergic, have been used totreat UI (See, e.g., A. J. Wein, Urol. Clin. N. Am. 22:557-577 (1995);Levin et al., J. Urol. 128:396-398 (1982); Cooke et al., S. Afr. Med. J.63:3 (1983); R. K. Mirakhur et al., Anaesthesia 38:1195-1204 (1983)).These drugs are not effective, however, in all patients havinguninhibited bladder contractions. Administration of anticholinergicmedications represent the mainstay of this type of treatment.

None of the existing commercial drug treatments for UI, however, hasachieved complete success in all classes of UI patients, nor hastreatment occurred without significant adverse side effects. Forexample, drowsiness, dry mouth, constipation, blurred vision, headaches,tachycardia, and cardiac arrhythmia, which are related to theanticholinergic activity of traditional anti-UI drugs, can occurfrequently and adversely affect patient compliance. Yet despite theprevalence of unwanted anticholinergic effects in many patients,anticholinergic drugs are currently prescribed for patients having UI.The Merck Manual of Medical Information 631-634 (R. Berkow ed., 1997).

Ulcers are sores occurring where the lining of the digestive tract hasbeen eroded by stomach acids or digestive juices. The sores aretypically well-defined round or oval lesions primarily occurring in thestomach and duodenum. About 1 in 10 people develop an ulcer. Ulcersdevelop as a result of an imbalance between acid-secretory factors, alsoknown as “aggressive factors,” such as stomach acid, pepsin, andHelicobacter pylori infection, and local mucosal-protective factors,such as secretion of bicarbonate, mucus, and prostaglandins.

Treatment of ulcers typically involves reducing or inhibiting theaggressive factors. For example, antacids such as aluminum hydroxide,magnesium hydroxide, sodium bicarbonate, and calcium bicarbonate can beused to neutralize stomach acids. Antacids, however, can causealkalosis, leading to nausea, headache, and weakness. Antacids can alsointerfere with the absorption of other drugs into the blood stream andcause diarrhea.

H₂ antagonists, such as cimetidine, ranitidine, famotidine, andnizatidine, are also used to treat ulcers. H₂ antagonists promote ulcerhealing by reducing gastric acid and digestive-enzyme secretion elicitedby histamine and other H₂ agonists in the stomach and duodenum. H₂antagonists, however, can cause breast enlargement and impotence in men,mental changes (especially in the elderly), headache, dizziness, nausea,myalgia, diarrhea, rash, and fever.

H⁺, K⁺—ATPase inhibitors such as omeprazole and lansoprazole are alsoused to treat ulcers. H⁺, K⁺—ATPase inhibitors inhibit the production ofenzymes used by the stomach to secrete acid. Side effects associatedwith H⁺, K⁺—ATPase inhibitors include nausea, diarrhea, abdominal colic,headache, dizziness, somnolence, skin rashes, and transient elevationsof plasma activities of aminotransferases.

Sucraflate is also used to treat ulcers. Sucraflate adheres toepithelial cells and is believed to form a protective coating at thebase of an ulcer to promote healing. Sucraflate, however, can causeconstipation, dry mouth, and interfere with the absorption of otherdrugs.

Antibiotics are used when Helicobacter pylori is the underlying cause ofthe ulcer. Often antibiotic therapy is coupled with the administrationof bismuth compounds such as bismuth subsalicylate and colloidal bismuthcitrate. The bismuth compounds are believed to enhance secretion ofmucous and HCO₃ ⁻, inhibit pepsin activity, and act as an antibacterialagainst H. pylori. Ingestion of bismuth compounds, however, can lead toelevated plasma concentrations of Bi⁺³ and can interfere with theabsorption of other drugs.

Prostaglandin analogues, such as misoprostal, inhibit secretion of acidand stimulate the secretion of mucous and bicarbonate and are also usedto treat ulcers, especially ulcers in patients who require nonsteroidalanti-inflammatory drugs. Effective oral doses of prostaglandinanalogues, however, can cause diarrhea and abdominal cramping. Inaddition, some prostaglandin analogues are abortifacients.

Carbenoxolone, a mineral corticoid, can also be used to treat ulcers.Carbenoxolone appears to alter the composition and quantity of mucous,thereby enhancing the mucosal barrier. Carbenoxolone, however, can leadto Na⁺ and fluid retention, hypertension, hypokalemia, and impairedglucose tolerance.

Muscarinic cholinergic antagonists such as pirenzapine and telenzapinecan also be used to reduce acid secretion and treat ulcers. Side effectsof muscarinic cholinergic antagonists include dry mouth, blurred vision,and constipation. The Merck Manual of Medical Information 496-500 (R.Berkow ed., 1997) and Goodman and Gilman's The Pharmacological Basis ofTherapeutics 901-915 (J. Hardman and L. Limbird eds., 9^(th) ed. 1996).

IBD is a chronic disorder in which the bowel becomes inflamed, oftencausing recurring abdominal cramps and diarrhea. The two types of IBDare Crohn's disease and ulcerative colitis.

Crohn's disease, which can include regional enteritis, granulomatousileitis, and ileocolitis, is a chronic inflammation of the intestinalwall. Crohn's disease occurs equally in both sexes and is more common inJews of eastern-European ancestry. Most cases of Crohn's disease beginbefore age 30 and the majority start between the ages of 14 and 24. Thedisease typically affects the full thickness of the intestinal wall.Generally the disease affects the lowest portion of the small intestine(ileum) and the large intestine, but can occur in any part of thedigestive tract.

Early symptoms of Crohn's disease are chronic diarrhea, crampy abdominalpain, fever, loss of appetite, and weight loss. Complications associatedwith Crohn's disease include the development of intestinal obstructions,abnormal connecting channels (fistulas), and abscesses. The risk ofcancer of the large intestine is increased in people who have Crohn'sdisease. Often Crohn's disease is associated with other disorders suchas gallstones, inadequate absorption of nutrients, amyloidosis,arthritis, episcleritis, aphthous stomatitis, erythema nodosum, pyodermagangrenosum, ankylosing spondylitis, sacroilitis, uveitis, and primarysclerosing cholangitis. There is no known cure for Crohn's disease.

Cramps and diarrhea, side effects associated with Crohn's disease, canbe relieved by anticholinergic drugs, diphenoxylate, loperamide,deodorized opium tincture, or codeine. Generally, the drug is takenorally before a meal.

Broad-spectrum antibiotics are often administered to treat the symptomsof Crohn's disease. The antibiotic metronidazole is often administeredwhen the disease affects the large intestine or causes abscesses andfistulas around the anus. Long-term use of metronidazole, however, candamage nerves, resulting in pins-and-needles sensations in the arms andlegs. Sulfasalazine and chemically related drugs can suppress mildinflammation, especially in the large intestine. These drugs, however,are less effective in sudden, severe flare-ups. Corticosteroids, such asprednisone, reduce fever and diarrhea and relieve abdominal pain andtenderness. Long-term corticosteroid therapy, however, invariablyresults in serious side effects such as high blood-sugar levels,increased risk of infection, osteoporosis, water retention, andfragility of the skin. Drugs such as azathioprine and mercaptourine cancompromise the immune system and are often effective for Crohn's diseasein patients that do not respond to other drugs. These drugs, however,usually need 3 to 6 months before they produce benefits and can causeserious side effects such as allergy, pancreatitis, and lowwhite-blood-cell count.

When Crohn's disease causes the intestine to be obstructed or whenabscesses or fistulas do not heal, surgery can be necessary to removediseased sections of the intestine. Surgery, however, does not cure thedisease, and inflammation tends to recur where the intestine isrejoined. In almost half of the cases a second operation is needed. TheMerck Manual of Medical Information 528-530 (R. Berkow ed., 1997).

Ulcerative colitis is a chronic disease in which the large intestinebecomes inflamed and ulcerated, leading to episodes of bloody diarrhea,abdominal cramps, and fever. Ulcerative colitis usually begins betweenages 15 and 30; however, a small group of people have their first attackbetween ages 50 and 70. Unlike Crohn's disease, ulcerative colitis neveraffects the small intestine and does not affect the full thickness ofthe intestine. The disease usually begins in the rectum and the sigmoidcolon and eventually spreads partially or completely through out thelarge intestine. The cause of ulcerative colitis is unknown.

Treatment of ulcerative colitis is directed to controlling inflammation,reducing symptoms, and replacing lost fluids and nutrients.Anticholinergic drugs and low doses of diphenoxylate or loperamide areadministered for treating mild diarrhea. For more intense diarrheahigher doses of diphenoxylate or loperamide, or deodorized opiumtincture or codeine are administered. Sulfasalazine, olsalazie,prednisone, or mesalamine can be used to reduce inflammation.Azathioprine and mercaptopurine have been used to maintain remissions inulcerative-colitis patients who would otherwise need long-termcorticosteroid treatment. In severe cases of ulcerative colitis thepatient is hospitalized and given corticosteroids intravenously. Peoplewith severe rectal bleeding can require transfusions and intravenousfluids. If toxic colitis develops and treatments fail, surgery to removethe large intestine can be necessary. Non-emergency surgery can beperformed if cancer is diagnosed, precancerous legions are detected, orunremitting chronic disease would otherwise make the person an invalidor dependent on high doses of corticosteroids. Complete removal of thelarge intestine and rectum permanently cures ulcerative colitis. TheMerck Manual of Medical Information 530-532 (R. Berkow ed., 1997) andGoodman and Gilman's The Pharmacological Basis of Therapeutics (J.Hardman and L. Limbird eds., 9^(th) ed. 1996).

IBS is a disorder of motility of the entire gastrointestinal tract,causing abdominal pain, constipation, and/or diarrhea. IBS affectsthree-times more women than men. In IBS stimuli such as stress, diet,drugs, hormones, or irritants can cause the gastrointestinal tract tocontract abnormally. During an episode of IBS contractions of thegastrointestinal tract become stronger and more frequent, resulting inthe rapid transit of food and feces through the small intestine, oftenleading to diarrhea. Cramps result from the strong contractions of thelarge intestine and increased sensitivity of pain receptors in the largeintestine.

There are two major types of IBS. The first type, spastic-colon type, iscommonly triggered by eating, and usually produces periodic constipationand diarrhea with pain. Mucous often appears in the stool. The pain cancome in bouts of continuous dull aching pain or cramps, usually in thelower abdomen. The person suffering from spastic-colon type IBS can alsoexperience bloating, gas, nausea, headache, fatigue, depression,anxiety, and difficulty concentrating. The second type of IBS usuallyproduces painless diarrhea or constipation. The diarrhea can beginsuddenly and with extreme urgency. Often the diarrhea occurs soon aftera meal and can sometimes occur immediately upon awakening.

Treatment of IBS typically involves modification of an IBS-patient'sdiet. Often it is recommended that an IBS patient avoid beans, cabbage,sorbitol, and fructose. A low-fat, high-fiber diet can also help someIBS patients. Regular physical activity can also help keep thegastrointestinal tract functioning properly. Drugs such as propanthelinethat slow the function of the gastrointestinal tract are generally noteffective for treating IBS. Antidiarrheal drugs, such as diphenoxylateand loperamide, help with diarrhea. The Merck Manual of MedicalInformation 525-526 (R. Berkow ed., 1997).

Many drugs can cause physical and/or psychological addiction. Those mostwell known types of these drugs include opiates, such as heroin, opium,and morphine; sympathomimetics, including cocaine and amphetamines;sedative-hypnotics, including alcohol, benzodiazepines and barbiturates;and nicotine, which has effects similar to opioids and sympathomimetics.Drug addiction is characterized by a craving or compulsion for takingthe drug and an inability to limit its intake. Additionally, drugdependence is associated with drug tolerance, the loss of effect of thedrug following repeated administration, and withdrawal, the appearanceof physical and behavioral symptoms when the drug is not consumed.Sensitization occurs if repeated administration of a drug leads to anincreased response to each dose. Tolerance, sensitization, andwithdrawal are phenomena evidencing a change in the central nervoussystem resulting from continued use of the drug. This change canmotivate the addicted individual to continue consuming the drug despiteserious social, legal, physical and/or professional consequences. (See,e.g., U.S. Pat. No. 6,109,269 to Rise et al.).

Certain pharmaceutical agents have been administered for treatingaddiction. U.S. Pat. No. 5,556,838 to Mayer et al. discloses the use ofnontoxic NMDA-blocking agents co-administered with an addictivesubstance to prevent the development of tolerance or withdrawalsymptoms. U.S. Pat. No. 5,574,052 to Rose et al. disclosesco-administration of an addictive substance with an antagonist topartially block the pharmacological effects of the substance. U.S. Pat.No. 5,075,341 to Mendelson et al. discloses the use of a mixed opiateagonist/antagonist to treat cocaine and opiate addiction. U.S. Pat. No.5,232,934 to Downs discloses administration of 3-phenoxypyridine totreat addiction. U.S. Pat. Nos. 5,039,680 and 5,198,459 to Imperato etal. disclose using a serotonin antagonist to treat chemical addiction.U.S. Pat. No. 5,556,837 to Nestler et. al. discloses infusing BDNF orNT-4 growth factors to inhibit or reverse neurological adaptive changesthat correlate with behavioral changes in an addicted individual. U.S.Pat. No. 5,762,925 to Sagan discloses implanting encapsulated adrenalmedullary cells into an animal's central nervous system to inhibit thedevelopment of opioid intolerance. U.S. Pat. No. 6,204,284 to Beer etal. discloses racemic(±)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane for use in theprevention or relief of a withdrawal syndrome resulting from addictionto drugs and for the treatment of chemical dependencies.

Parkinson's disease is a clinical syndrome comprising bradykinesia(slowness and poverty of movement), muscular rigidity, resting tremor(which usually abates during voluntary movement), and an impairment ofpostural balance leading to disturbance of gait and falling. Thefeatures of Parkinson's disease are a loss of pigmented, dopaminergicneurons of the substantia nigra pars compacta and the appearance ofintracellular inclusions known as Lewy bodies (Goodman and Gillman's ThePharmaceutical Basis of Therapeutics 506 (9^(th) ed. 1996)). Withouttreatment, Parkinson's disease progresses to a rigid akinetic state inwhich patients are incapable of caring for themselves. Death frequentlyresults from complications of immobility, including aspiration pneumoniaor pulmonary embolism. Drugs commonly used for the treatment ofParkinson's disease include carbidopa/levodopa, pergolide,bromocriptine, selegiline, amantadine, and trihexyphenidylhydrochloride. There remains, however, a need for drugs useful for thetreatment of Parkinson's disease and having an improved therapeuticprofile.

Anxiety is a fear, apprehension, or dread of impending danger oftenaccompanied by restlessness, tension, tachycardia, and dyspnea. Othersymptoms commonly associated with anxiety include depression, especiallyaccompanied with dysthymic disorder (chronic “neurotic” depression);panic disorder; agoraphobia and other specific phobias; eatingdisorders; and many personality disorders. Often anxiety is unattachedto a clearly identified treatable primary illness. If a primary illnessis found, however, it can be desirable to deal with the anxiety at thesame time as the primary illness.

Currently, benzodiazepines are the most commonly used anti-anxietyagents for generalized anxiety disorder. Benzodiazepines, however, carrythe risk of producing impairment of cognition and skilled motorfunctions, particularly in the elderly, which can result in confusion,delerium, and falls with fractures. Sedatives are also commonlyprescribed for treating anxiety. The azapirones, such as buspirone, arealso used to treat moderate anxiety. The azapirones, however, are lessuseful for treating severe anxiety accompanied with panic attacks.

Epilepsy is a disorder characterized by the tendency to have recurringseizures. The etiology commonly consists of lesions in some part of thecortex, such as a tumor; developmental malformation; or damage due totrauma or stroke. In some cases the etiology is genetic. An epilepticseizure can be triggered by repetitive sounds, flashing lights, videogames, or touching certain parts of the body. Epilepsy is typicallytreated with anti-seizure drugs. In epilepsy cases, where anti-seizuredrugs are ineffective, and the defect in the brain is isolated to asmall area of the brain, surgical removal of that part of the brain canbe helpful in alleviating the seizures. In patients who have severalsources for the seizures or who have seizures that spread quickly to allparts of the brain, surgical removal of the nerve fibers that connectthe two sides of the brain can be helpful.

Examples of drugs for treating a seizure and epilepsy includecarbamazepine, ethosuximide, gabapentin, lamotrignine, phenobarbital,phenytoin, primidone, valproic acid, trimethadione, bemzodiaepines,γ-vinyl GABA, acetazolamide, and felbamate. Anti-seizure drugs, however,can have side effects such as drowsiness; hyperactivity; hallucinations;inability to concentrate; central and peripheral nervous systemtoxicity, such as nystagmus, ataxia, diplopia, and vertigo; gingivalhyperplasia; gastrointestinal disturbances such as nausea, vomiting,epigastric pain, and anorexia; endocrine effects such as inhibition ofantidiuretic hormone, hyperglycemia, glycosuria, osteomalacia; andhypersensitivity such as scarlatiniform rash, morbilliform rash,Stevens-Johnson syndrome, systemic lupus erythematosus, and hepaticnecrosis; and hematological reactions such as red-cell aplasia,agranulocytosis, thrombocytopenia, aplastic anemia, and megaloblasticanemia. The Merck Manual of Medical Information 345-350 (R. Berkow ed.,1997).

A seizure is the result of abnormal electrical discharge in the brain.The discharge can involve a small area of the brain and lead to theperson only noticing an odd taste or smell or it can involve a largearea of the brain and lead to convulsions, i.e., a seizure that causesjerking and spasms of the muscles throughout the body. Convulsions canalso result in brief attacks of altered consciousness and loss ofconsciousness, muscle control, or bladder control. A seizures is oftenpreceded by auras, i.e., unusual sensations of smell, taste, or visionor an intense feeling that a seizure is about to begin. A seizuretypically lasts for about 2 to 5 minutes. When the seizure ends theperson can have headache, sore muscles, unusual sensations, confusion,and profound fatigue (postictal state). Usually the person cannotremember what happened during the seizure.

A stroke or cerebrovascular accident, is the death of brain tissue(cerebral infarction) resulting from the lack of blood flow andinsufficient oxygen to the brain. A stroke can be either ischemic orhemorrhagic. In an ischemic stroke, blood supply to the brain is cut offbecause of athersclerosis or a blood clot that has blocked a bloodvessel. In a hemorrhagic stroke, a blood vessel bursts preventing normalblood flow and allowing blood to leak into an area of the brain anddestroying it. Most strokes develop rapidly and cause brain damagewithin minutes. In some cases, however, strokes can continue to worsenfor several hours or days. Symptoms of strokes vary depending on whatpart of the brain is effected. Symptoms include loss or abnormalsensations in an arm or leg or one side of the body, weakness orparalysis of an arm or leg or one side of the body, partial loss ofvison or hearing, double vision, dizziness, slurred speech, difficultyin thinking of the appropriate word or saying it, inability to recognizeparts of the body, unusual movements, loss of bladder control,imbalance, and falling, and fainting. The symptoms can be permanent andcan be associated with coma or stupor. Strokes can cause edema orswelling of the brain which can further damage brain tissue. For personssuffering from a stroke, intensive rehabilitation can help overcome thedisability caused by impairment of brain tissue. Rehabilitation trainsother parts of the brain to assume the tasks previously performed by thedamaged part.

Examples of drugs for treating strokes include anticoagulants such asheparin, drugs that break up clots such as streptokinase or tissueplasminogen activator, and drugs that reduce swelling such as mannitolor corticosteroids. The Merck Manual of Medical Information 352-355 (R.Berkow ed., 1997).

Pruritus is an unpleasant sensation that prompts scratching. Prurituscan be attributed to dry skin, scabies, dermatitis, herpetiformis,atopic dermatitis, pruritus vulvae et ani, miliaria, insect bites,pediculosis, contact dermatitis, drug reactions, urticaria, urticarialeruptions of pregnancy, psoriasis, lichen planus, lichen simplexchronicus, exfoliative dermatitis, folliculitis, bullous pemphigoid, andfiberglass dermatitis. Conventionally, pruritus is treated byphototherapy with ultraviolet B or PUVA or with therapeutic agents suchas naltrexone, nalmefene, danazol, tricyclics, and antidepressants.

Selective antagonists of the metabotropic glutamate receptor 5(“mGluR5”) have been shown to exert analgesic activity in in vivo animalmodels (K. Walker et al., Neuropharmacology 40:1-9 (2000) and A. Dogrulet al., Neuroscience Letters, 292(2): 115-118 (2000)).

Selective antagonists of the mGluR5 receptor have also been shown toexert anxiolytic and anti-depressant activity in in vivo animal models(E. Tatarczynska et al., Br. J. Pharmacol. 132(7):1423-1430 (2001) andP. J. M. Will et al., Trends in Pharmacological Sciences 22(7):331-37(2001)).

Selective antagonists of the mGluR5 receptor have also been shown toexert anti-Parkinson activity in vivo (K. J. Ossowska et al.,Neuropharmacology 41(4):413-20 (2001) and P. J. M. Will et al., Trendsin Pharmacological Sciences 22(7):331-37 (2001)).

Selective antagonists of the mGluR5 receptor have also been shown toexert anti-dependence activity in vivo (C. Chiamulera et al., NatureNeuroscience 4(9):873-74 (2001)).

U.S. Pat. No. 6,150,129 to Cook et al. describes a class of dinitrogenheterocycles useful as antibiotics.

U.S. Pat. No. 5,529,998 to Habich et al. describes a class ofbenzooxazolyl- and benzothiazolyloxazolidones useful as antibacterials.

International publication no. WO 01/57008 describes a class of2-benzothiazolyl urea derivatives useful as inhibitors ofserine/threonine and tyrosine kinases.

International publication no. WO 02/08221 describes aryl piperazinecompounds useful for treating chronic and acute pain conditions, itch,and urinary incontinence.

International publication no. WO 99/37304 describes substitutedoxoazaheterocycly compounds useful for inhibiting factor Xa.

International publication no. WO 00/59510 describes aminopyrimidinesuseful as sorbitol dehydrogenase inhibitors.

Japanese patent application no. 11-199573 to Kiyoshi et al. describesbenzothiazole derivatives that are neuronal 5HT3 receptor agonists inthe intestinal canal nervous system and useful for treating digestivedisorders and pancreatic insufficiency.

German patent application no 199 34 799 to Rainer et al. describes achiral-smectic liquid crystal mixture containing compounds with 2 linked(hetero)aromatic rings or compounds with 3 linked (hetero)aromaticrings.

M. Chu-Moyer et al., J. Med. Chem. 45:511-528 (2002) describesheterocycle-substituted piperazino-pyrimidines useful as sorbitoldehydrogenase inhibitors.

B. G. Khadse et al., Bull. Haff. Instt. 1(3):27-32 (1975) describes2-(N⁴-substituted-N¹-piperazinyl)pyrido(3,2-d)thiazoles and5-nitro-2-(N⁴-substituted-N¹-piperazinyl)benzthiazoles useful asanthelmintic agents.

There remains, however, a clear need in the art for new drugs useful fortreating or preventing pain, UI, an ulcer, IBD, IBS, an addictivedisorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke,a seizure, a pruritic condition, psychosis, a cognitive disorder, amemory deficit, restricted brain function, Huntington's chorea, ALS,dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia,or depression.

Citation of any reference in Section 2 of this application is not to beconstrued as an admission that such reference is prior art to thepresent application.

3. SUMMARY OF THE INVENTION

The present invention encompasses compounds having the formula (Ia):

and pharmaceutically acceptable salts thereof, wherein

-   -   Ar₁ is

-   -   A is

-   -   R₁ is —Cl, —Br, —I, —(C₁-C₆)alkyl, —NO₂, —CN, —OH, —OCH₃, —NH₂,        —C(halo)₃, —CH(halo)₂, or —CH₂(halo);    -   each R² is independently:        -   (a) -halo, —CN, —OH, —O(C₁-C₆)alkyl, —NO₂, or —NH₂;        -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,            —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,            —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,            —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to            7-membered)heterocycle, or -(7- to            10-membered)bicycloheterocycle, each of which is            unsubstituted or substituted with one or more R₅ groups; or        -   (c) -phenyl, -naphthyl, —(C₁₄)aryl, or -(5- to            10-membered)heteroaryl, each of which is unsubstituted or            substituted with one or more R₆ groups;    -   each R₃ is independently:        -   (a) -halo, —CN, —OH, —O(C₁-C₆)alkyl, —NO₂, or —NH₂;        -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,            —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,            —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,            —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to            7-membered)heterocycle, or -(7- to            10-membered)bicycloheterocycle, each of which is            unsubstituted or substituted with one or more R₅ groups; or        -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to            10-membered)heteroaryl, each of which is unsubstituted or            substituted with one or more R₆ groups;    -   R₄ is —H or —(C₁-C₆)alkyl;    -   each R₅ is independently —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,        —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇,        —SR₇, —S(O)R_(—7), or —S(O)₂R₇;    -   each R₆ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,        —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl,        -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃, —CH(halo)₂, —CH₂(halo),        —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,        —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or        —S(O)₂R₇;    -   each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,        —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl,        -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃, —CH₂(halo), or        —CH(halo)₂;    -   R₈ and R₉ are each independently —H, —(C₁-C₆)alkyl,        —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,        —(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃, —CH(halo)₂,        —CH₂(halo), —OC(halo)₃, —OCH(halo)₂, —OCH₂(halo), —CN, —OH,        -halo, —N₃, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,        —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;    -   each -halo is —F, —Cl, —Br,— or —I;    -   n is an integer ranging from 0 to 3;    -   p is an integer ranging from 0 to 2;    -   m is 0 or 1; and    -   x is 0 or 1.

The present invention encompasses compounds having the formula (Ib):

and pharmaceutically acceptable salts thereof, wherein

-   -   Ar₁ is

-   -   A is

-   -   R₁ is —H, -halo, —(C₁-C₆)alkyl, —NO₂, —CN, —OH, —OCH₃, —NH₂,        —C(halo)₃, —CH(halo)₂, or —CH₂(halo);    -   each R² is independently:        -   (a) -halo, —CN, —OH, —O(C₁-C₆)alkyl, —NO₂, or —NH₂;        -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,            —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,            —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,            —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to            7-membered)heterocycle, or -(7- to            10-membered)bicycloheterocycle, each of which is            unsubstituted or substituted with one or more R₅ groups; or        -   (c) -phenyl, -naphthyl, —(C₁₄)aryl, or -(5- to            10-membered)heteroaryl, each of which is unsubstituted or            substituted with one or more R₆ groups;    -   each R₃ is independently:        -   (a) -halo, —CN, —OH, —O(C₁-C₆)alkyl, —NO₂, or —NH₂;        -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,            —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,            —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,            —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to            7-membered)heterocycle, or -(7- to            10-membered)bicycloheterocycle, each of which is            unsubstituted or substituted with one or more R₅ groups; or        -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to            10-membered)heteroaryl, each of which is unsubstituted or            substituted with one or more R₆ groups;    -   R₄ is —H or —(C₁-C₆)alkyl;    -   each R₅ is independently —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,        —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇,        —SR₇, —S(O)R₇, or —S(O)₂R₇;    -   each R₆ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,        —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl,        -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃, —CH(halo)₂, —CH₂(halo),        —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,        —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or        —S(O)₂R₇;    -   each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,        —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl,        -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃, —CH₂(halo), or        —CH(halo)₂;    -   R₈ and R₉ are each independently —H, —(C₁-C₆)alkyl,        —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,        —(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃, —CH(halo)₂,        —CH₂(halo), —OC(halo)₃, —OCH(halo)₂, —OCH₂(halo), —CN, —OH,        -halo, —N₃, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,        —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;    -   each -halo is —F, —Cl, —Br,— or —I;    -   p is an integer ranging from 0 to 2;    -   m is 0 or 1; and    -   x is 0 or 1.

The present invention encompasses compounds having the formula (IIa):

and pharmaceutically acceptable salts thereof, wherein

-   -   R₁ is —Cl, —Br, —I, —(C₁-C₆)alkyl, —NO₂, —CN, —OH, —OCH₃, —NH₂,        —C(halo)₃, —CH(halo)₂, or —CH₂(halo);    -   each R² is independently:        -   (a) -halo, —CN, —OH, —O(C₁-C₆)alkyl, —NO₂, or —NH₂;        -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,            —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,            —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,            —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to            7-membered)heterocycle, or -(7- to            10-membered)bicycloheterocycle, each of which is            unsubstituted or substituted with one or more R₅ groups; or        -   (c) -phenyl, -naphthyl, —(C₁₄)aryl, or -(5- to            10-membered)heteroaryl, each of which is unsubstituted or            substituted with one or more R₆ groups;    -   each R₃ is independently:        -   (a) -halo, —CN, —OH, —O(C₁-C₆)alkyl, —NO₂, or —NH₂;        -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,            —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,            —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,            —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to            7-membered)heterocycle, or -(7- to            10-membered)bicycloheterocycle, each of which is            unsubstituted or substituted with one or more R₅ groups; or        -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to            10-membered)heteroaryl, each of which is unsubstituted or            substituted with one or more R₆ groups;    -   each R₅ is independently —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,        —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇,        —SR₇, —S(O)R₇, or —S(O)₂R₇;    -   each R₆ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,        —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl,        -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃, —CH(halo)₂, —CH₂(halo),        —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,        —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or        —S(O)₂R₇;    -   each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,        —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl,        -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃, —CH₂(halo), or        —CH(halo)₂;    -   R₈ and R₉ are each independently —H, —(C₁-C₆)alkyl,        —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,        —(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃, —CH(halo)₂,        —CH₂(halo), —OC(halo)₃, —OCH(halo)₂, —OCH₂(halo), —CN, —OH,        -halo, —N₃, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,        —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;    -   R₁₀ is —H or —(C₁-C₄)alkyl;    -   each -halo is —F, —Cl, —Br,— or —I;    -   n is an integer ranging from 0 to 3;    -   p is an integer ranging from 0 to 2; and    -   m is 0 or 1.

The present invention encompasses compounds having the formula (IIb):

and pharmaceutically acceptable salts thereof, wherein

-   -   Ar₁ is

-   -   A is

-   -   R₁ is —H, -halo, —(C₁-C₆)alkyl, —NO₂, —CN, —OH, —OCH₃, —NH₂,        —C(halo)₃, —CH(halo)₂, or —CH₂(halo);    -   each R² is independently:        -   (a) -halo, —CN, —OH, —O(C₁-C₆)alkyl, —NO₂, or —NH₂;        -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,            —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,            —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,            —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to            7-membered)heterocycle, or -(7- to            10-membered)bicycloheterocycle, each of which is            unsubstituted or substituted with one or more R₅ groups; or        -   (c) -phenyl, -naphthyl, —(C₁₄)aryl, or -(5- to            10-membered)heteroaryl, each of which is unsubstituted or            substituted with one or more R₆ groups;    -   each R₃ is independently:        -   (a) -halo, —CN, —OH, —O(C₁-C₆)alkyl, —NO₂, or —NH₂;        -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,            —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,            —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,            —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to            7-membered)heterocycle, or -(7- to            10-membered)bicycloheterocycle, each of which is            unsubstituted or substituted with one or more R₅ groups; or        -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to            10-membered)heteroaryl, each of which is unsubstituted or            substituted with one or more R₆ groups;    -   R₄ is —H or —(C₁-C₆)alkyl;    -   each R₅ is independently —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,        —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇,        —SR₇, —S(O)R₇, or —S(O)₂R₇;    -   each R₆ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,        —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl,        -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃, —CH(halo)₂, —CH₂(halo),        —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,        —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or        —S(O)₂R₇;    -   each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,        —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl,        -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃, —CH₂(halo), or        —CH(halo)₂;    -   R₈ and R₉ are each independently —H, —(C₁-C₆)alkyl,        —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,        —(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃, —CH(halo)₂,        —CH₂(halo), —OC(halo)₃, —OCH(halo)₂, —OCH₂(halo), —CN, —OH,        -halo, —N₃, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,        —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;    -   R₁₀ is —H or —(C₁-C₄)alkyl;    -   each -halo is —F, —Cl, —Br,— or —I;    -   p is an integer ranging from 0 to 2;    -   m is 0 or 1; and    -   x is 0 or 1.

The present invention encompasses compounds having the formula (IIIa):

and pharmaceutically acceptable salts thereof, wherein

-   -   Ar₁ is

-   -   A is

-   -   R₁ is —Cl, —Br, —I, —(C₁-C₆)alkyl, —NO₂, —CN, —OH, —OCH₃, —NH₂,        —C(halo)₃, —CH(halo)₂, or —CH₂(halo);    -   each R² is independently:        -   (a) -halo, —CN, —OH, —O(C₁-C₆)alkyl, —NO₂, or —NH₂;        -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,            —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,            —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,            —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to            7-membered)heterocycle, or -(7- to            10-membered)bicycloheterocycle, each of which is            unsubstituted or substituted with one or more R₅ groups; or        -   (c) -phenyl, -naphthyl, —(C₁₄)aryl, or -(5- to            10-membered)heteroaryl, each of which is unsubstituted or            substituted with one or more R₆ groups;    -   each R₃ is independently:        -   (a) -halo, —CN, —OH, —O(C₁-C₆)alkyl, —NO₂, or —NH₂;        -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,            —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,            —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,            —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to            7-membered)heterocycle, or -(7- to            10-membered)bicycloheterocycle, each of which is            unsubstituted or substituted with one or more R₅ groups; or        -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to            10-membered)heteroaryl, each of which is unsubstituted or            substituted with one or more R₆ groups;    -   R₄ is —H or —(C₁-C₆)alkyl;    -   each R₅ is independently —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,        —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇,        —SR₇, —S(O)R₇, or —S(O)₂R₇;    -   each R₆ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,        —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl,        -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃, —CH(halo)₂, —CH₂(halo),        —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,        —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or        —S(O)₂R₇;    -   each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,        —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl,        -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃, —CH₂(halo), or        —CH(halo)₂;    -   R₈ and R₉ are each independently —H, —(C₁-C₆)alkyl,        —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,        —(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃, —CH(halo)₂,        —CH₂(halo), —OC(halo)₃, —OCH(halo)₂, —OCH2(halo), —CN, —OH,        -halo, —N₃, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,        —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;    -   each -halo is —F, —Cl, —Br,— or —I;    -   n is an integer ranging from 0 to 3;    -   p is an integer ranging from 0 to 2;    -   m is 0 or 1; and    -   x is 0 or 1.

The present invention encompasses compounds having the formula (IIIb):

and pharmaceutically acceptable salts thereof, wherein

-   -   Ar₁ is

-   -   A is

-   -   R₁ is —H, -halo, —(C₁-C₆)alkyl, —NO₂, —CN, —OH, —OCH₃, —NH₂,        —C(halo)₃, —CH(halo)₂, or —CH₂(halo);    -   each R² is independently:        -   (a) -halo, —CN, —OH, —O(C₁-C₆)alkyl, —NO₂, or —NH₂;        -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,            —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,            —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,            —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, or -(7-            to 10-membered)bicycloheterocycle, each of which is            unsubstituted or substituted with one or more R₅ groups; or        -   (c) -phenyl, -naphthyl, or —(C₁₄)aryl each of which is            unsubstituted or substituted with one or more R₆ groups;    -   each R₃ is independently:        -   (a) -halo, —CN, —OH, —O(C₁-C₆)alkyl, —NO₂, or —NH₂;        -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,            —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,            —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,            —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to            7-membered)heterocycle, or -(7- to            10-membered)bicycloheterocycle, each of which is            unsubstituted or substituted with one or more R₅ groups; or        -   (c) -phenyl, -naphthyl, —(C₁₄)aryl or -(5- to            10-membered)heteroaryl, each of which is unsubstituted or            substituted with one or more R₆ groups;    -   R₄ is —H or —(C₁-C₆)alkyl;    -   each R₅ is independently —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,        —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇,        —SR₇, —S(O)R₇, or —S(O)₂R₇;    -   each R₆ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,        —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl,        -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃, —CH(halo)₂, —CH₂(halo),        —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,        —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or        —S(O)₂R₇;    -   each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,        —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl,        -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃, —CH₂(halo), or        —CH(halo)₂;    -   R₈ and R₉ are each independently —H, —(C₁-C₆)alkyl,        —(C₂-₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,        —(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃, —CH(halo)₂,        —CH₂(halo), —OC(halo)₃, —OCH(halo)₂, —OCH₂(halo), —CN, —OH,        -halo, —N₃, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,        —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;    -   each -halo is —F, —Cl, —Br,— or —I;    -   p is an integer ranging from 0 to 2;    -   m is 0 or 1; and    -   x is 0 or 1.

The present invention also encompasses compounds having the formula(IVa):

and pharmaceutically acceptable salts thereof, wherein

-   -   Ar₁ is

-   -   Ar₂ is

-   -   R₁ is -halo, —(C₁-C₆)alkyl, —NO₂, —CN, —OH, —OCH₃, —NH₂,        —C(halo)₃, —CH(halo)₂, or —CH₂(halo);    -   each R² is independently:        -   (a) -halo, —CN, —OH, —O(C₁-C₆)alkyl, —NO₂, or —NH₂;        -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,            —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,            —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,            —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to            7-membered)heterocycle, or -(7- to            10-membered)bicycloheterocycle, each of which is            unsubstituted or substituted with one or more R₅ groups; or        -   (c) -phenyl, -naphthyl, —(C₁₄)aryl, or -(5- to            10-membered)heteroaryl, each of which is unsubstituted or            substituted with one or more R₆ groups;    -   R₃ is —H or —CH₃:    -   each R₅ is independently —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,        —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇,        —SR₇, —S(O)R₇, or —S(O)₂R₇;    -   each R₆ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,        —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl,        -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃, —CH(halo)₂, —CH₂(halo),        —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,        —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or        —S(O)₂R₇;    -   each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,        —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl,        -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃, —CH₂(halo), or        —CH(halo)₂;    -   R₈ and R₉ are each independently —H, —(C₁-C₆)alkyl,        —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,        —(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃, —CH(halo)₂,        —CH₂(halo), —OC(halo)₃, —OCH(halo)₂, —OCH₂(halo), —CN, —OH,        -halo, —N₃, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,        —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;    -   each -halo is —F, —Cl, —Br,— or —I;    -   n is an integer ranging from 0 to 3; and    -   p is an integer ranging from 0 to 2.

The present invention also encompasses compounds having the formula(IVb):

and pharmaceutically acceptable salts thereof, wherein

-   -   Ar₁ is

-   -   Ar₂ is

-   -   A is

-   -   R₁ is -halo, —(C₁-C₆)alkyl, —NO₂, —CN, —OH, —OCH₃, —NH₂,        —C(halo)₃, —CH(halo)₂, or —CH₂(halo);    -   each R² is independently:        -   (a) -halo, —CN, —OH, —O(C₁-C₆)alkyl, —NO₂, or —NH₂;        -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,            —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,            —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,            —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to            7-membered)heterocycle, or -(7- to            10-membered)bicycloheterocycle, each of which is            unsubstituted or substituted with one or more R₅ groups; or        -   (c) -phenyl, -naphthyl, —(C₁₄)aryl, or -(5- to            10-membered)heteroaryl, each of which is unsubstituted or            substituted with one or more R₆ groups;    -   R₃ is —CH₃;    -   R₄ is —H or —(C₁-C₆)alkyl;    -   each R₅ is independently —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,        —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇,        —SR₇, —S(O)R₇, or —S(O)₂R₇;    -   each R₆ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,        —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl,        -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃, —CH(halo)₂, —CH₂(halo),        —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,        —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or        —S(O)₂R₇;    -   each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,        —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl,        -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃, —CH₂(halo), or        —CH(halo)₂;    -   R₈ and R₉ are each independently —H, —(C₁-C₆)alkyl,        —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,        —(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃, —CH(halo)₂,        —CH₂(halo), —OC(halo)₃, —OCH(halo)₂, —OCH₂(halo), —CN, —OH,        -halo, —N₃, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,        —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;    -   each -halo is —F, —Cl, —Br,— or —I;    -   n is an integer ranging from 0 to 3;    -   p is an integer ranging from 0 to 2; and    -   x is 0 or 1.

The present invention also encompasses compounds having the formula (V):

and pharmaceutically acceptable salts thereof, wherein

-   -   Ar₁ is

-   -   Ar₂ is

-   -   R₁ is -halo, —(C₁-C₆)alkyl, —NO₂, —CN, —OH, —OCH₃, —NH₂,        —C(halo)₃, —CH(halo)₂, or —CH₂(halo);    -   each R² is independently:        -   (a) -halo, —CN, —OH, —O(C₁-C₆)alkyl, —NO₂, or —NH₂;        -   (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,            —(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl,            —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,            —(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to            7-membered)heterocycle, or -(7- to            10-membered)bicycloheterocycle, each of which is            unsubstituted or substituted with one or more R₅ groups; or        -   (c) -phenyl, -naphthyl, —(C₁₄)aryl, or -(5- to            10-membered)heteroaryl, each of which is unsubstituted or            substituted with one or more R₆ groups;    -   R₃ is —H or —CH₃:    -   each R₅ is independently —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂,        —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇,        —SR₇, —S(O)R₇, or —S(O)₂R₇;    -   each R₆ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,        —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl,        -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃, —CH(halo)₂, —CH₂(halo),        —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇,        —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or        —S(O)₂R₇;    -   each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,        —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl,        -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃, —CH₂(halo), or        —CH(halo)₂;    -   R₈ and R₉ are each independently —H, —(C₁-C₆)alkyl,        —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,        —(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃, —CH(halo)₂,        —CH₂(halo), —OC(halo)₃, —OCH(halo)₂, —OCH₂(halo), —CN, —OH,        -halo, —N₃, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,        —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;    -   each -halo is —F, —Cl, —Br,— or —I;    -   n is an integer ranging from 0 to 3; and    -   p is an integer ranging from 0 to 2.

A compound of formula (Ia), (Ib), (IIa), (IIb), (IIIa), (IIIb), (IVa),(IVb), and (V) or a pharmaceutically acceptable salt thereof (a“Benzoazolylpiperazine Compound”) is useful for treating or preventingpain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson'sdisease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruriticcondition, psychosis, a cognitive disorder, a memory deficit, restrictedbrain function, Huntington's chorea, ALS, dementia, retinopathy, amuscle spasm, a migraine, vomiting, dyskinesia, or depression in ananimal.

The invention also relates to compositions comprising an effectiveamount of a Benzoazolylpiperazine Compound and a pharmaceuticallyacceptable carrier or excipient. The compositions are useful fortreating or preventing pain, UI, an ulcer, IBD, IBS, an addictivedisorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke,a seizure, a pruritic condition, psychosis, a cognitive disorder, amemory deficit, restricted brain function, Huntington's chorea, ALS,dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia,or depression in an animal.

The invention further relates to methods for treating pain, UI, anulcer, IBD, IBS, an addictive disorder, Parkinson's disease,parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruriticcondition, psychosis, a cognitive disorder, a memory deficit, restrictedbrain function, Huntington's chorea, ALS, dementia, retinopathy, amuscle spasm, a migraine, vomiting, dyskinesia, or depression comprisingadministering to an animal in need thereof an effective amount of aBenzoazolylpiperazine Compound.

The invention further relates to methods for preventing pain, UI, anulcer, IBD, IBS, an addictive disorder, Parkinson's disease,parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruriticcondition, psychosis, a cognitive disorder, a memory deficit, restrictedbrain function, Huntington's chorea, ALS, dementia, retinopathy, amuscle spasm, a migraine, vomiting, dyskinesia, or depression comprisingadministering to an animal in need thereof an effective amount of aBenzoazolylpiperazine Compound.

The invention still further relates to methods for inhibiting VanilloidReceptor 1 (“VR1”) function in a cell, comprising contacting a cellcapable of expressing VR1 with an effective amount of aBenzoazolylpiperazine Compound.

The invention still further relates to methods for inhibiting mGluR₅function in a cell, comprising contacting a cell capable of expressingmGluR₅ with an effective amount of a Benzoazolylpiperazine Compound.

The invention still further relates to methods for inhibitingmetabotropic glutamate receptor 1 (“mGluR1”) function in a cell,comprising contacting a cell capable of expressing mGluR1 with aneffective amount of a Benzoazolylpiperazine Compound.

The invention still further relates to a method for preparing acomposition comprising the step of admixing a BenzoazolylpiperazineCompound and a pharmaceutically acceptable carrier or excipient.

The invention still further relates to a kit comprising a containercontaining an effective amount of a Benzoazolylpiperazine Compound.

The present invention still further relates to a compound selected fromthe group consisting of

and pharmaceutically acceptable salts thereof.

The present invention still further relates to a compound selected fromthe group consisting of

and pharmaceutically acceptable salts thereof.

The present invention still further relates to a compound selected fromthe group consisting of

and pharmaceutically acceptable salts thereof.

The present invention can be understood more fully by reference to thefollowing detailed description and illustrative examples, which areintended to exemplify non-limiting embodiments of the invention.

4. DETAILED DESCRIPTION OF THE INVENTION 4.1 The Compounds of Formula(Ia)

As stated above, the present invention encompasses compounds of Formula(Ia)

and pharmaceutically acceptable salts thereof, where Ar₁, R₃, R₈, R₉, A,x, and m, are defined above for the Benzoazolylpiperazine Compounds offormula (Ia).

In one embodiment, Ar₁ is a pyridyl group.

In another embodiment, Ar₁ is a pyrimidinyl group.

In another embodiment, x is 1 and A is —C(O)—N(R₄)—.

In another embodiment, x is 1 and A is —C(S)—N(R₄)—.

In another embodiment x is 0.

In another embodiment, n or p is 0.

In another embodiment, n or p is 1.

In another embodiment, m is 0.

In another embodiment, m is 1.

In another embodiment, R₄ is —H.

In another embodiment, R₄ is —(C₁-C₆)alkyl.

In another embodiment, Ar₁ is a pyridyl group, x is 1, and A is—C(O)N(R₄)—.

In another embodiment, Ar₁ is a pyridyl group, x is 1, and A is—C(S)N(R₄)—.

In another embodiment, Ar₁ is a pyrimidinyl group, x is 1, and A is—(O)N(R₄)—.

In another embodiment, Ar₁ is a pyrimidinyl group, x is 1, and A is—C(S)N(R₄)—.

In another embodiment, R₁ is —Cl.

In another embodiment, R₁ is —Br.

In another embodiment, R₁ is —I.

In another embodiment, R₁ is —(C₁-C₆)alkyl.

In another embodiment, R₁ is —CH₃.

In another embodiment, R₁ is —NO₂.

In another embodiment, R₁ is —CN.

In another embodiment, R₁ is —OH.

In another embodiment, R₁ is —OCH₃.

In another embodiment, R₁ is —NH₂.

In another embodiment, R₁ is —C(halo)₃.

In another embodiment, R₁ is —CH(halo)₂.

In another embodiment, R₁ is —CH₂(halo).

In another embodiment, n and p are 1 and R₂ is -halo, —CN, —OH,—O(C₁-C₆)alkyl, —NO₂, or —NH₂.

In another embodiment, n and p are 1 and R₂ is —(C₁-C₁₀)alkyl,—(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl,—(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,—(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, eachof which is unsubstituted or substituted with one or more R₅ groups.

In another embodiment, n and p are 1 and R₂ is -phenyl, -naphthyl,—(C₁₄)aryl, or -(5- to 10-membered)heteroaryl, each of which isunsubstituted or substituted with one or more R₆ groups;

In another embodiment, m is 1 and R₃ is -halo, —CN, —OH, —O(C₁-C₆)alkyl,—NO₂, or —NH₂.

In another embodiment, m is 1 and R₃ is —(C₁-C₁₀)alkyl,—(C₂—C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl,—(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,—(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, eachof which is unsubstituted or substituted with one or more R₅ groups.

In another embodiment, m is 1 and R₃ is -phenyl, -naphthyl, —(C₁₄)arylor -(5- to 10-membered)heteroaryl, each of which is unsubstituted orsubstituted with one or more R₆ groups.

In another embodiment, R₈ and R₉ are each independently —H, -halo,—(C₁-C₆)alkyl, —O(C₁-C₆)alkyl, —C(halo)₃, —CH(halo)₂, or —CH₂(halo).

In another embodiment, at least one of R₈ and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or, —I; x is1; A is —C(O)—N(R₄)—; R₄ is —H; and R₈ and R₉ are —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, and R₈ and R₉ are —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 1;A is —C(O)—N(R₄)—; is —H; R₈ is —H; R₈ is —H; and R₉ is -halo. Inanother embodiment, R₁ is —Cl. In another embodiment, R₉ is —Cl. Inanother embodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -halo. In anotherembodiment, R₁ is —Cl. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 1;A is —C(O)—N(R₄)—; R₄ is —H; R₈ is -halo; and R₉ is —H. In anotherembodiment, R₁ is —Cl. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -halo, and R₉ is —H. In anotherembodiment, R₁ is —Cl. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 1;A is —C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is —CH₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₁ is —CH₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 1;A is —C(O)—N(R₄)—; R₄ is —H; R₈ is —CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CH₃, and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 1;A is —C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is —CF₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is —CF₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 1;A is —C(O)—N(R₄)—; R₄ is —H; R₈ is —CF₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —CF₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 1;A is —C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is —OCH₂CH₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is —OCH₂CH₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 1;A is —C(O)—N(R₄)—; R₄ is —H; R₈ is —OCH₂CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —OCH₂CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; and R₈ and R₉ are —H.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is -halo. In anotherembodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. In anotherembodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is -halo; and R₉ is —H. In anotherembodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. In anotherembodiment, R₈ is —F.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is —CH₃.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is —CF₃.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —CF₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is —OCH₂CH₃.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —OCH₂CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; and R₈ and R₉ are —H.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is -halo. In anotherembodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. In anotherembodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is -halo; and R₉ is —H. In anotherembodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. In anotherembodiment, R₈ is —F.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is —CH₃.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is —CF₃.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —CF₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is —OCH₂CH₃.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —OCH₂CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 1;A is —C(O)—N(R₄)—; R₄ is —H; R₈ is -tert-butyl; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is -tert-butyl; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is R₁ is —Cl —Br, or —I; xis 1; A is —C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is -tert-butyl.

In another embodiment, n, p, and m are 0; R₁ is R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is -tert-butyl.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is -tert-butyl; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is -tert-butyl.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —CH₃; and R₉ is —CH₃.

In another embodiment, n is 0, Ar₁ is -2-(3-nitropyridyl)-, m is 0, x is0, and R₈ and R₉ are —H.

In another embodiment, n is 0, Ar₁ is -2-(3-chloropyridyl)-, x is 1, Ais —C(S)—N(R₄)—, m is 1, R₃ is —CH₃, R₃ is attached to the carbon atomadjacent to the nitrogen attached to the —C(SO)—N(R₄)— group, the carbonatom to which the R₃ group is attached has the R configuration, R₈ is—H, and R₉ is —CH₃.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 1; A is —C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group;and R₈ and R₉ are —H. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, and R₈ andR₉ are —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 1; A is —C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group;R₈ is —H; and R₉ is -halo. In another embodiment R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —Cl x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is -halo. In another embodiment R₉ is —Cl. In another embodiment,R₉ is —Br. In another embodiment, R₉ is —F. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.In another embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 1; A is —C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group;R₈ is -halo; and R₉ is —H. In another embodiment R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —Cl x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is-halo, and R₉ is —H. In another embodiment R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 1; A is —C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group;R₈ is —H; and R₉ is —CH₃. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —Cl x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 1; A is —C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group;R₈ is —CH₃; and R₉ is —H. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —Cl x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CH₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 1; A is —C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group;R₈ is —H; and R₉ is —CF₃. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CF₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 1; A is —C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group;R₈ is —CF₃; and R₉ is —H. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —Cl x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CF₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 1; A is —C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group;R₈ is —H; and R₉ is —OCH₂CH₃. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —OCH₂CH₃. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 1; A is —C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group;R₈ is —OCH₂CH₃; and R₉ is —H. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is—OCH₂CH₃, and R₉ is —H. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, and R₈ andR₉ are —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is -halo. In another embodiment R₉ is —Cl. In another embodiment,R₉ is —Br. In another embodiment, R₉ is —F. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.In another embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is-halo, and R₉ is —H. In another embodiment R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CH₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CF₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CF₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₉ is —H,and R₉ is —OCH₂CH₃. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is—OCH₂CH₃, and R₉ is —H. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, and R₈ andR₉ are —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is -halo. In another embodiment R₉ is —Cl. In another embodiment,R₉ is —Br. In another embodiment, R₉ is —F. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.In another embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is-halo, and R₉ is —H. In another embodiment R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CH₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CF₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CF₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —OCH₂CH₃. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is—OCH₂CH₃, and R₉ is —H. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 1; A is —C(O)—N(R₄)—; R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group; R₄ is —H;R₈ is -tert-butyl; and R₉ is —H. In another embodiment, the carbon atomto which the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group, R₄ is —H, R₁ is-tert-butyl, and R₉ is —H. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 1; A is —C(O)—N(R₄)—; R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group; R₄ is —H;R₈ is —H; and R₉ is -tert-butyl. In another embodiment, the carbon atomto which the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group, R₄ is —H, R₈ is —H, andR₉ is -tert-butyl. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group, R₄ is —H, R₈ is-tert-butyl, and R₉ is —H. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group, R₄ is —H, R₈ is —H, andR₉ is -tert-butyl. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group, R₄ is —H, R₈ is —CH₃,and R₉ is —CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or, —I; x is0; R₄ is —H; and R₈ and R₉ are —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 0; R₄ is —H;and R₈ and R₉ are —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or, —I; x is0; R₄ is —H; R₈ is —H; and R₉ is -halo. In another embodiment, R₉ is—Cl. In another embodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 0; R₄ is —H;R₈ is —H; and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or, —I; x is0; R₄ is —H; R₈ is -halo; and R₉ is —H. In another embodiment, R₈ is—Cl. In another embodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, n, p, and m are 0; R₁ is -C₁; x is 0; R₄ is —H;R₈ is -halo; and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or, —I; x is0; R₄ is —H; R₈ is —H; and R₉ is —CH₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 0; R₄ is —H;R₈ is —H; and R₉ is —CH₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or, —I; x is0; R₄ is —H; R₈ is —CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 0; R₄ is —H;R₈ is —CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or, —I; x is0; R₄ is —H; R₈ is —H; and R₉ is —CF₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 0; R₄ is —H;R₈ is —H; and R₉ is —CF₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or, —I; x is0; R₄ is —H; R₈ is —CF₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 0; R₄ is —H;R₈ is —CF₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or, —I; x is0; R₄ is —H; R₈ is —H; and R₉ is —OCH₂CH₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 0; R₄ is —H;R₈ is —H; and R₉ is —OCH₂CH₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or, —I; x is0; R₄ is —H; R₈ is —OCH₂CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 0; R₄ is —H;R₈ is —OCH₂CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; x is 0; R₄ is —H;and R₈ and R₉ are —H.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; x is 0; R₄ is —H;R₈ is —H; and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; x is 0; R₄ is —H;R₈ is -halo; and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; x is 0; R₄ is —H;R₈ is —H; and R₉ is —CH₃.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; x is 0; R₄ is —H;R₈ is —CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; x is 0; R₄ is —H;R₈ is —H; and R₉ is —CF₃.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; x is 0; R₄ is —H;R₈ is —CF₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; x is 0; R₄ is —H;R₈ is —H; and R₉ is —OCH₂CH₃.

In another embodiment, n, p, and m are 0, R₁ is —CH₃; x is 0; R₄ is —H;R₈ is —OCH₂CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; x is 0; R₄ is —H;and R₈ and R₉ are —H.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; x is 0; R₄ is —H;R₈ is —H; and R₉ is -halo. In another embodiment, R₈ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; x is 0; R₄ is —H;R₈ is -halo; and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; x is 0; R₄ is —H;R₈ is —H; and R₉ is —CH₃.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; x is 0; R₄ is —H;R₈ is —CF₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; x is 0; R₄ is —H;R₈ is —H; and R₉ is —CF₃.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; x is 0; R₄ is —H;R₈ is —CF₃; and and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; x is 0; R₄ is —H;R₈ is —H; and R₉ is —OCH₂CH₃.

In another embodiment, n, p, and m are 0, R₁ is —CF₃; x is 0; R₄ is —H;R₈ is —OCH₂CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or, —I; x is0; R₄ is —H; R₈ is -tert-butyl; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 0; R₄ is —H;R₈ is -tert-butyl; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or, —I; x is0; R₄ is —H; R₈ is —H; and R₉ is -tert-butyl.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 0; R₄ is —H;R₈ is —H; and R₉ is -tert-butyl.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; x is 0; R₄ is —H;R₈ is -tert-butyl; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; x is 0; R₄ is —H;R₈ is —H; and R₉ is -tert-butyl.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; x is 0; R₄ is —H;R₈ is —CH₃; and R₉ is —CH₃.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 0; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atom adjacentto the nitrogen attached to the benzothiazolyl group; and R₈ and R₉ are—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; x is 0; R₄ is—H; R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group; and R₈ and R₉ are —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 0; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atom adjacentto the nitrogen attached to the benzothiazolyl group; R₈ is —H; and R₉is -halo. In another embodiment R₉ is —Cl. In another embodiment, R₉ is—Br. In another embodiment, R₉ is —F. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, n and pare 0, m is 1, R₁ is —Cl, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group, R₈ is —H, and R₉ is-halo. In another embodiment R₉ is —Cl. In another embodiment, R₉ is—Br. In another embodiment, R₉ is —F. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 0; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atom adjacentto the nitrogen attached to the benzothiazolyl group; R₈ is -halo; andR₉ is —H. In another embodiment R₈ is —Cl. In another embodiment, R₈ is—Br. In another embodiment, R₈ is —F. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —Cl, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benxothiazolyl group, R₈ is -halo, and R₉ is—H. In another embodiment R₈ is —Cl. In another embodiment, R₈ is —Br.In another embodiment, R₈ is —F. In another embodiment, the carbon atomto which the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 0; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atom adjacentto the nitrogen attached to the benzothiazxolyl group; R₈ is —H; and R₉is —C₃. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —Cl, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazxolyl group; R₈ is —H; and R₉ is —C₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 0; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atom adjacentto the nitrogen attached to the benzothiazolyl group; R₈ is —CH₃; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —Cl, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group, R₈ is —CH₃, and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 0; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atom adjacentto the nitrogen attached to the benzothiazolyl group; R₈ is —H; and R₉is —CF₃. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —Cl, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group; R₈ is —H; and R₉ is —CF₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 0; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atom adjacentto the nitrogen attached to the benzothiazolyl group; R₈ is —CF₃; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —Cl, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group, R₈ is —CF₃, and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 0; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atom adjacentto the nitrogen attached to the benzothiazolyl group; R₈ is —H; and R₉is —OCH₂CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —Cl, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group, R₈ is —H, and R₉ is—OCH₂CH₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 0; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atom adjacentto the nitrogen attached to the benzothiazolyl group; R₈ is —OCH₂CH₃;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —Cl, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group, R₈ is —H, and R₉ is—OCH₂CH₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group, and R₈ and R₉ are —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group, R₈ is —H, and R is -halo.In another embodiment R₉ is —Cl. In another embodiment, R₉ is —Br. Inanother embodiment, R₉ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group, R₈ is -halo, and R₉ is—H. In another embodiment R₈ is —Cl. In another embodiment, R₈ is —Br.In another embodiment, R₈ is —F. In another embodiment, the carbon atomto which the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R,is —CH₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group, R₈ is —H, and R₉ is —CH₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group, R₈ is —CH₃, and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group, R₈ is —H, and R₉ is —CF₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group, R₈ is —CF₃, and R is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group, R₈ is —H, and R₉ is—OCH₂CH₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group, R₈ is —OCH₂CH₃, and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group, and R₈ and R₉ are —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group, R₈ is —H, and R₉ is-halo. In another embodiment R₉ is —Cl. In another embodiment, R₉ is—Br. In another embodiment, R₉ is —F. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group, R₈ is -halo, and R₉ is—H. In another embodiment R₈ is —Cl. In another embodiment, R₈ is —Br.In another embodiment, R₈ is —F. In another embodiment, the carbon atomto which the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group, R₈ is —H, and R₉ is —CH₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group, R₈ is —CH₃, and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group, R₈ is —H, and R₉ is —CF₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group, R₈ is —CF₃, and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group, R₈ is —H, and R₉ is—OCH₂CH₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group, R₈ is —OCH₂CH₃, and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 0; R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group; R₄ is —H; R₈ is-tert-butyl; and R is —H. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —Cl, x is 0, R₃ is—CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₄ is —H, R₈ is -tert-butyl, andR₉ is —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or, —I; xis 0; R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzothiazolyl group; R₄ is —H; R₈ is —H; andR₉ is -tert-butyl. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —Cl, x is 0, R₃ is—CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₄ is —H, R₈ is —H, and R is-tert-butyl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 0, R₃ is—CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₄ is —H, R₈ is -tert-butyl, andR₉ is —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 0, R₃ is—CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₄ is —H, R₈ is —H, and R₉ is-tert-butyl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 0, R₃ is—CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₄ is —H, R₈ is —CH₃, and R₉ is—CH₃. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; m is 1; R is—CH₃, —Cl, —Br, or —I; x is 1; A is —C(O)—N(R₄)—; R₃ is —CH₃ and isattached to the carbon atom adjacent to the nitrogen attached to the—C(O)—N(R₄)— group; R₄ is —H; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —Cl. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyridyl group; n is 0; m is 1; R₁ is—Cl, —Br, or —I; x is 1; A is —C(O)—N(R₄)—; R₃ is —CH₃ and is attachedto the carbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)—group; R₄ is —H; R₈ is —H; and R₉ is —Br. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.In another embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0, m is 1, R₁ is—Cl, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbonatom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₄ is—H, R₈ is —H, and R₉ is —Br. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyridyl group, n is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —F. In another embodiment, the carbon atomto which the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyrimidinyl group; p is 0; m is 1; R is—CH₃, —Cl, —Br, or —I; x is 1; A is —C(O)—N(R₄)—; R₃ is —CH₃ and isattached to the carbon atom adjacent to the nitrogen attached to the—C(O)—N(R₄)— group; R₄ is —H; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —Cl. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group; p is 0; m is 1; R₁ is—Cl, —Br, or —I; x is 1; A is —C(O)—N(R₄)—; R₃ is —CH₃ and is attachedto the carbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)—group; R₄ is —H; R₈ is —H; and R₉ is —Br. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.In another embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0, m is 1, R₁ is—Cl, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbonatom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₄ is—H, R₈ is —H, and R₉ is —Br. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —F. In another embodiment, the carbon atomto which the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyridyl group; n is 0; m is 1; R₁ is—CH₃, —Cl, —Br, or —I; x is 0; R₃ is —CH₃ and is attached to the carbonatom adjacent to the nitrogen attached to the benzothiazolyl group; R₄is —H; R₈ is —H; and R₉ is -halo. In another embodiment, the carbon atomto which the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyridyl group, n is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzothiazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Cl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group; n is 0; m is 1; R₁ is—Cl, —Br, or —I; x is 0; R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the benzothiazolyl group; R₄ is —H;R₈ is —H; and R₉ is —Br. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyridyl group, n is 0, m is 1, R₁ is—Cl, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzothiazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Br. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzothiazolyl group, R₄ is —H, R₈ is —H,and R₉ is —F. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group; p is 0; m is 1; R₁ is—CH₃, —Cl, —Br, or —I; x is 0; R₃ is —CH₃ and is attached to the carbonatom adjacent to the nitrogen attached to the benzothiazolyl group; R₄is —H; R₁ is —H; and R₉ is -halo. In another embodiment, the carbon atomto which the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzothiazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Cl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group; p is 0; m is 1; R₁ is—Cl, —Br, or —I; x is 0; R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the benzothiazolyl group; R₄ is —H;R₈ is —H; and R₉ is —Br. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0, m is 1, R₁ is—Cl, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzothiazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Br. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzothiazolyl group, R₄ is —H, R₈ is —H,and R₉ is —F. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)—when x is 1 or the benzothiazolyl group when x is 0. In anotherembodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached to the carbonatom adjacent to the nitrogen attached to the —C(O)—N(R₄)— when x is 1or the benzothiazolyl group when x is 0 and the carbon to which the R₃group is attached is in the R configuration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— when xis 1 or the benzothiazolyl group when x is 0. In another embodiment, mis 1 and R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the —C(O)—N(R₄)— when x is 1 or the benzothiazolylgroup when x is 0 and the carbon to which the R₃ group is attached is inthe R configuration.

In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)—when x is 1 or the benzothiazolyl group when x is 0. In anotherembodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached to the carbonatom adjacent to the nitrogen attached to the —C(O)—N(R₄)— when x is 1or the benzothiazolyl group when x is 0 and the carbon to which the R₃group is attached is in the S configuration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— when xis 1 or the benzothiazolyl group when x is 0. In another embodiment, mis 1 and R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the —C(O)—N(R₄)— when x is 1 or the benzothiazolylgroup when x is 0 and the carbon to which the R₃ group is attached is inthe S configuration.

In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the pyridyl groupor pyrimidinyl group. In another embodiment, m is 1 and R₃ is—(C₁-C₄)alkyl and is attached to the carbon atom adjacent to thenitrogen attached to the pyridyl group or pyrimidinyl group and thecarbon to which the R₃ group is attached is in the R configuration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the pyridyl group orpyrimidinyl group. In another embodiment, m is 1 and R₃ is —CH₃ and isattached to the carbon atom adjacent to the nitrogen attached to thepyridyl group or pyrimidinyl group and the carbon to which the R₃ groupis attached is in the R configuration.

In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the pyridyl groupor pyrimidinyl group. In another embodiment, im is 1 and R₃ is—(C₁-C₄)alkyl and is attached to the carbon atom adjacent to thenitrogen attached to the pyridyl group or pyrimidinyl group and thecarbon to which the R₃ group is attached is in the S configuration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the pyridyl group orpyrimidinyl group. In another embodiment, m is 1 and R₃ is —CH₃ and isattached to the carbon atom adjacent to the nitrogen attached to thepyridyl group or pyrimidinyl group and the carbon to which the R₃ groupis attached is in the S configuration.

4.2 The Compounds of Formula (Ib)

The present invention also encompasses compounds of formula (Ib):

and pharmaceutically acceptable salts thereof, where Ar₁, R₃, R₈, R₉, A,x, and m, are defined above for the Benzoazolylpiperazine Compounds offormula (Ib).

In one embodiment, Ar₁ is a pyrazinyl group.

In another embodiment, Ar₁ is a pyridazinyl group.

In another embodiment, Ar₁ is a thiazanyl group.

In another embodiment, x is 1 and A is —C(O)—N(R₄)—.

In another embodiment, x is 1 and A is —C(S)—N(R₄)—.

In another embodiment x is 0.

In another embodiment, p is 0.

In another embodiment, p is 1.

In another embodiment, m is 0.

In another embodiment, m is 1.

In another embodiment, R₄ is —H.

In another embodiment, R₄ is —(C₁-C₆)alkyl.

In another embodiment, Ar₁ is a pyrazinyl group, x is 1, and A is—C(O)N(R₄)—.

In another embodiment, Ar₁ is a pyrazinyl group, x is 1, and A is—C(S)N(R₄)—.

In another embodiment, Ar₁ is a pyridazinyl group, x is 1, and A is—C(O)N(R₄)—.

In another embodiment, Ar₁ is a pyridazinyl group, x is 1, and A is—C(S)N(R₄)—.

In another embodiment, Ar₁ is a thiazanyl group, x is 1, and A is—C(O)N(R₄)—.

In another embodiment, Ar₁ is a thiazanyl group, x is 1, and A is—C(S)N(R₄)—.

In another embodiment, R₁ is —H.

In another embodiment, R₁ is —Cl.

In another embodiment, R₁ is —Br.

In another embodiment, R₁ is —I.

In another embodiment, R₁ is —F.

In another embodiment, R₁ is —(C₁-C₆)alkyl.

In another embodiment, R₁ is —CH₃.

In another embodiment, R₁ is —NO₂.

In another embodiment, R₁ is —CN.

In another embodiment, R₁ is —OH.

In another embodiment, R₁ is —OCH₃.

In another embodiment, R₁ is —NH₂.

In another embodiment, R₁ is —C(halo)₃.

In another embodiment, R₁ is —CH(halo)₂.

In another embodiment, R₁ is —CH₂(halo).

In another embodiment, p is 1 and R₂ is -halo, —CN, —OH, —O(C₁-C₆)alkyl,—NO₂, or —NH₂.

In another embodiment, p is 1 and R₂ is —(C₁-C₁₀)alkyl,—(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl,—(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,—(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, eachof which is unsubstituted or substituted with one or more R₅ groups.

In another embodiment, p is 1 and R₂ is -phenyl, -naphthyl, —(C₁₄)aryl,or -(5- to 10-membered)heteroaryl, each of which is unsubstituted orsubstituted with one or more R₆ groups.

In another embodiment, m is 1 and R₃ is -halo, —CN, —OH, —O(C₁-C₆)alkyl,—NO₂, or —NH₂.

In another embodiment, m is 1 and R₃ is —(C₁-C₁₀)alkyl,—(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl,—(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,—(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, eachof which is unsubstituted or substituted with one or more R₅ groups.

In another embodiment, m is 1 and R₃ is -phenyl, -naphthyl, —(C₁₄)arylor -(5- to 10-membered)heteroaryl, each of which is unsubstituted orsubstituted with one or more R₆ groups.

In another embodiment, R₈ and R₉ are each independently —H, halo,—(C₁-C₆)alkyl, —O(C₁-C₆)alkyl, —C(halo)₃, —CH(halo)₂, or —CH₂(halo).

In another embodiment, at least one of R₈ or R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, and R₈ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, and R₈ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -halo. In anotherembodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. In anotherembodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -halo. In anotherembodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. In anotherembodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -halo, and R₁ is —H. In anotherembodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. In anotherembodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -halo, and R₉ is —H. In anotherembodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. In anotherembodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is -halo x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CH3, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is -halo x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is -halo x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, and R₈ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -halo. In anotherembodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. In anotherembodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -halo, and R₉ is —H. In anotherembodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. In anotherembodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, and R₈ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -halo. In anotherembodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. In anotherembodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -halo, and R₉ is —H. In anotherembodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. In anotherembodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -tert-butyl, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -tert-butyl, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -tert-butyl.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -tert-butyl.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -tert-butyl, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -tert-butyl.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CH₃, and R₉ is —CH₃.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, and R₈ andR₉ are —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, and R₈ andR₉ are —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is-halo, and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is-halo, and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₁ is —H,and R₉ is —CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₁ is —H,and R₉ is —CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CH₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CH₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CF₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CF₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CF₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CF₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —OCH₂CH₃. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —OCH₂CH₃. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is—OCH₂CH₃, and R₉ is —H. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is—OCH₂CH₃, and R₉ is —H. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, and R₈ andR₉ are —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is -halo. In another embodiment R₉ is —Cl. In another embodiment,R₉ is —Br. In another embodiment, R₉ is —F. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.In another embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is-halo, and R₉ is —H. In another embodiment R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CH₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CF₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CF₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —OCH₂CH₃. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is—OCH₂CH₃, and R₉ is —H. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, and R₈ andR₉ are —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is -halo. In another embodiment R₉ is —Cl. In another embodiment,R₉ is —Br. In another embodiment, R₉ is —F. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.In another embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is-halo, and R₉ is —H. In another embodiment R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CH₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CF₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CF₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —OCH₂CH₃. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is—OCH₂CH₃, and R₉ is —H. In another embodiment, the carbon atom o whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—(R₄)— group, R₄ is —H, R₈ is-tert-butyl, and R₉ is —H. In another embodiment, the carbon tom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—(R₄)— group, R₄ is —H, R₈ is-tert-butyl, and R₉ is —H. In another embodiment, the carbon tom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—(R₄)— group, R₄ is —H, R₈ is —H, andR₉ is -tert-butyl. In another embodiment, the carbon tom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—(R₄)— group, R₄ is —H, R₈ is —H, andR₉ is -tert-butyl. In another embodiment, the carbon tom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—(R₄)— group, R₄ is —H, R₈ is-tert-butyl, and R₉ is —H. In another embodiment, the carbon tom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—(R₄)— group, R₄ is —H, R₈ is —H, andR₉ is -tert-butyl. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group, R₄ is —H, R₈ is —CH₃,and R₉ is —CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p and m are 0, R₁ is -halo x is 0, R₄ is —H, andR₈ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, andR₈ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is -halo x is 0, R₄ is —H, R₈is —H, and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—H, and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is -halo, and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is-halo, and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is —H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is —CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is —H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is —CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is —H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is —OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, andR₈ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —H, and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is -halo, and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, andR₈ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is —H, and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is -halo, and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is —H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is —CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is —H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is —CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is —H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is —OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is -tert-butyl, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is-tert-butyl, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is —H, and R₉ is -tert-butyl.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—H, and R₉ is -tert-butyl.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is -tert-butyl, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —H, and R₉ is -tert-butyl.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —CH₃, and R₉ is —CH₃.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —H, and R₉ is -halo. Inanother embodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. Inanother embodiment, R₉ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —H, and R₉ is -halo. Inanother embodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. Inanother embodiment, R₉ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is -halo, and R₉ is —H. Inanother embodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. Inanother embodiment, R₈ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is -halo, and R₉ is —H. Inanother embodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. Inanother embodiment, R₈ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —H, and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —H, and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —H, and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —H, and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —CF₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —CF₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —H, and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —H, and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —OCH₂CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —OCH₂CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —H, and R₉ is -halo. Inanother embodiment R₉ is —Cl. In another embodiment, R₉ is —Br. Inanother embodiment, R₉ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is -halo, and R₉ is —H. Inanother embodiment R₈ is —Cl. In another embodiment, R₈ is —Br. Inanother embodiment, R₈ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —H, and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —H, and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —CF₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —H, and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —OCH₂CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —H, and R₉ is -halo. Inanother embodiment R₉ is —Cl. In another embodiment, R₉ is —Br. Inanother embodiment, R₉ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is -halo, and R₉ is —H. Inanother embodiment R₈ is —Cl. In another embodiment, R₈ is —Br. In oneembodiment, R₈ is —F. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —H, and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —H, and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —CF₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —H, and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzothiazolyl group, R₈ is —OCH₂CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₃ is —CH₃and is attached to the carbon atom adjacent to the nitrogen attached tothe benzothiazolyl group, R₄ is —H, R₈ is -tert-butyl, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₃ is —CH₃ andis attached to the carbon atom adjacent to the nitrogen attached to thebenzothiazolyl group, R₄ is —H, R₈ is -tert-butyl, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₃ is —CH₃and is attached to the carbon atom adjacent to the nitrogen attached tothe benzothiazolyl group, R₄ is —H, R₈ is —H, and R₉ is -tert-butyl. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₃ is —CH₃ andis attached to the carbon atom adjacent to the nitrogen attached to thebenzothiazolyl group, R₄ is —H, R₈ is —H, and R₉ is -tert-butyl. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₃ is —CH₃and is attached to the carbon atom adjacent to the nitrogen attached tothe benzothiazolyl group, R₄ is —H, R₈ is -tert-butyl, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₃ is —CH₃and is attached to the carbon atom adjacent to the nitrogen attached tothe benzothiazolyl group, R₄ is —H, R₈ is —H, and R₉ is -tert-butyl. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₃ is —CH₃and is attached to the carbon atom adjacent to the nitrogen attached tothe benzothiazolyl group, R₄ is —H, R₈ is —CH₃, and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrazinyl group, p is 0, m is 1, R₁ is—CH₃ or -halo, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached tothe carbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)—group, R₄ is —H, R₈ is —H, and R₉ is -halo. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.In another embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyrazinyl group, p is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —Cl. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyrazinyl group, p is 0, m is 1, R₁ is-halo, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —Br. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyrazinyl group, p is 0, m is 1, R₁ is—Cl, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbonatom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₄ is—H, R₈ is —H, and R₉ is —Br. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyrazinyl group, p is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —F. In another embodiment, the carbon atomto which the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—CH₃ or -halo, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached tothe carbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)—group, R₄ is —H, R₈ is —H, and R₉ is -halo. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.In another embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —Cl. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is-halo, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —Br. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—Cl, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbonatom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₄ is—H, R₈ is —H, and R₉ is —Br. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —F. In another embodiment, the carbon atomto which the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—CH₃ or -halo, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached tothe carbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)—group, R₄ is —H, R₈ is —H, and R₉ is -halo. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.In another embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —Cl. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is-halo, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —Br. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—Cl, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbonatom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₄ is—H, R₈ is —H, and R₉ is —Br. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —F. In another embodiment, the carbon atomto which the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyrazinyl group, p is 0, m is 1, R₁ is—CH₃ or -halo, x is 0, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the benzothiazolyl group, R₄ is —H,R₈ is —H, and R₉ is -halo. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyrazinyl group, p is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzothiazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Cl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrazinyl group, p is 0, m is 1, R₁ is-halo, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzothiazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Br. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrazinyl group, p is 0, m is 1, R₁ is—Cl, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzothiazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Br. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrazinyl group, p is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzothiazolyl group, R₄ is —H, R₈ is —H,and R₉ is —F. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—CH₃ or -halo, x is 0, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the benzothiazolyl group, R₄ is —H,R₈ is —H, and R₉ is -halo. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzothiazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Cl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is-halo, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzothiazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Br. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—Cl, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzothiazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Br. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzothiazolyl group, R₄ is —H, R₈ is —H,and R₉ is —F. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—CH₃ or -halo, x is 0, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the benzothiazolyl group, R₄ is —H,R₈ is —H, and R₉ is -halo. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzothiazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Cl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is-halo, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzothiazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Br. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—Cl, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzothiazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Br. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzothiazolyl group, R₄ is —H, R₈ is —H,and R₉ is —F. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)—when x is 1 or the benzothiazolyl group when x is 0. In anotherembodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached to the carbonatom adjacent to the nitrogen attached to the —C(O)—N(R₄)— when x is 1or the benzothiazolyl group when x is 0 and the carbon to which the R₃group is attached is in the R configuration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— when xis 1 or the benzothiazolyl group when x is 0. In another embodiment, mis 1 and R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the —C(O)—N(R₄)— when x is 1 or the benzothiazolylgroup when x is 0 and the carbon to which the R₃ group is attached is inthe R configuration.

In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)—when x is 1 or the benzothiazolyl group when x is 0. In anotherembodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached to the carbonatom adjacent to the nitrogen attached to the —C(O)—N(R₄)— when x is 1or the benzothiazolyl group when x is 0 and the carbon to which the R₃group is attached is in the S configuration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— when xis 1 or the benzothiazolyl group when x is 0. In another embodiment, mis 1 and R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the —C(O)—N(R₄)— when x is 1 or the benzothiazolylgroup when x is 0 and the carbon to which the R₃ group is attached is inthe S configuration.

In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the pyrazinylgroup, pyridazinyl group, or a thiazanyl group. In another embodiment, mis 1 and R₃ is —(C₁-C₄)alkyl and is attached to the carbon atom adjacentto the nitrogen attached to the pyrazinyl group, pyridazinyl group, or athiazanyl group and the carbon to which the R₃ group is attached is inthe R configuration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the pyrazinyl group,pyridazinyl group, or thiazanyl group. In another embodiment, m is 1 andR₃ is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the pyrazinyl group, pyridazinyl group, or thiazanyl groupand the carbon to which the R₃ group is attached is in the Rconfiguration.

In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the pyrazinylgroup, pyridazinyl group, or thiazanyl group. In another embodiment, mis 1 and R₃ is —(C₁-C₄)alkyl and is attached to the carbon atom adjacentto the nitrogen attached to the pyrazinyl group, pyridazinyl group, orthiazanyl group and the carbon to which the R₃ group is attached is inthe S configuration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the pyrazinyl group,pyridazinyl group, or thiazanyl group. In another embodiment, m is 1 andR₃ is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the pyrazinyl group, pyridazinyl group, or thiazanyl groupand the carbon to which the R₃ group is attached is in the Sconfiguration.

The present invention also encompasses compounds of formula (IIa):

4.3 The Compounds of Formula (IIa)

and pharmaceutically acceptable salts thereof, where Ar₁, R₃, R₈, R₉,R₁₀ and m, are defined above for the Benzoazolylpiperazine Compounds offormula (IIa).

In one embodiment, Ar₁ is a pyridyl group.

In another embodiment, Ar₁ is a pyrimidinyl group.

In another embodiment, Ar₁ is a pyrazinyl group.

In another embodiment, n or p is 0.

In another embodiment, n or p is 1.

In another embodiment, m is 0.

In another embodiment, m is 1.

In another embodiment, R₁₀ is —H.

In another embodiment, R₁₀ is —(C₁-C₄)alkyl.

In another embodiment, R₁₀ is —CH₃.

In another embodiment, R₁ is —Cl.

In another embodiment, R₁ is —Br.

In another embodiment, R₁ is —I.

In another embodiment, R₁ is —(C₁-C₆)alkyl.

In another embodiment, R₁ is —CH₃.

In another embodiment, R₁ is —NO₂.

In another embodiment, R₁ is —CN.

In another embodiment, R₁ is —OH.

In another embodiment, R₁ is —OCH₃.

In another embodiment, R₁ is —NH₂.

In another embodiment, R₁ is —C(halo)₃.

In another embodiment, R₁ is —CH(halo)₂.

In another embodiment, R₁ is —CH₂(halo).

In another embodiment, n and p are 1 and R₂ is -halo, —CN, —OH,—O(C₁-C₆)alkyl, —NO₂, or —NH₂.

In another embodiment, n and p are 1 and R₂ is —(C₁-C₁₀)alkyl,—(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl,—(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,—(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, eachof which is unsubstituted or substituted with one or more R₅ groups.

In another embodiment, n and p are 1 and R₂ is -phenyl, -naphthyl,—(C₁₄)aryl, or -(5- to 10-membered)heteroaryl, each of which isunsubstituted or substituted with one or more R₆ groups;

In another embodiment, m is 1 and R₃ is -halo, —CN, —OH, —O(C₁-C₆)alkyl,—NO₂, or —NH₂,

In another embodiment, m is 1 and R₃ is —(C₁-C₁₀)alkyl,—(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl,—(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,—(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, eachof which is unsubstituted or substituted with one or more R₅ groups.

In another embodiment, m is 1 and R₃ is -phenyl, -naphthyl, —(C₁₄)arylor -(5- to 10-membered)heteroaryl, each of which is unsubstituted orsubstituted with one or more R₆ groups.

In another embodiment, R₈ and R₉ are each independently —H, halo,—(C₁-C₆)alkyl, —O(C₁-C₆)alkyl, —C(halo)₃, —CH(halo)₂, or —CH₂(halo).

In another embodiment, at least one of R₈ or R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; R₄ is—H; and R₈ and R₉ are —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, R₄ is —H; and R₈and R₉ are —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; R₄ is—H; R₈ is -halo H; and R₉ is —H. In another embodiment, R₉ is —Cl. Inanother embodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl; R₄ is —H; R₈ is-halo; and R₉ is —H. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; R₄ is—H; R₈ is —H; and R₉ is —CH₃. In another embodiment, R₉ is —Cl. Inanother embodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl, R₄ is —H; R₈ is —H;and R₉ is —CH₃. In another embodiment, R₉ is —Cl. In another embodiment,R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; R₄ is—H; R₈ is —CH₃; and R₉ is —H. In another embodiment, R₉ is —Cl. Inanother embodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl, R₄ is —H; R₈ is—CH₃; and R₉ is —H. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; R₄ is—H; R₈ is —H; and R₉ is —CF₃. In another embodiment, R₉ is —Cl. Inanother embodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl; R₄ is —H; R₈ is —H;and R₉ is —CF₃. In another embodiment, R₉ is —Cl. In another embodiment,R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; R₄ is—H; R₈ is —CF₃; and R₉ is —H. In another embodiment, R₉ is —Cl. Inanother embodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl; R₄ is —H; R₈ is—CF₃; and R₉ is —H. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; R₄ is—H; R₈ is —H; and R₉ is —OCH₂CH₃. In another embodiment, R₉ is —Cl. Inanother embodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl; R₄ is —H; R₈ is —H;and R₉ is —OCH₂CH₃. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; R₄ is—H; R₈ is —OCH₂CH₃; and R₉ is —H. In another embodiment, R₉ is —Cl. Inanother embodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl; R₄ is —H; R₈ is—OCH₂CH₃; and R₉ is —H. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl, Br, or —I; R₄ is—H; R₈ is —H; and R₉ is —CH₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl; R₄ is —H; R₈ is —H;and R₉ is —CH₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl, Br, or —I; R₄ is—H; R₈ is —CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl; R₄ is —H; R₈ is—CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, Br, or —I; R₄ is—H; R₈ is —H; and R₉ is —CF₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl; R₄ is —H; R₈ is —H;and R₉ is —CF₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl, Br, or —I; R₄ is—H; R₈ is —CF₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl; R₄ is —H; R₈ is—CF₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, Br, or —I; R₄ is—H; R₈ is —H; and R₉ is —OCH₂CH₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl; R₄ is —H; R₈ is —H;and R₉ is —OCH₂CH₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl, Br, or —I; R₄ is—H; R₈ is —OCH₂CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl; R₄ is —H; R₈ is—OCH₂CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0, R₁ is —CH₃, R₄ is —H, and R₈and R₉ are —H.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; R₄ is —H; R₈ is—H; and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; R₄ is —H; R₈ is-halo; and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; R₄ is —H; R₈ is—H; and R₉ is —CH₃.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; R₄ is —H; R₈ is—CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; R₄ is —H; R₈ is—H; and R₉ is —CF₃.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; R₄ is —H; R₁ is—CF₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; R₄ is —H; R₈ is—H; and R₉ is —OCH₂CH₃.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; R₄ is —H; R₈ is—OCH₂CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; R₄ is —H; and R₈and R₉ are —H.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; R₄ is —H; R₈ is—H; and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; R₄ is —H; R₈ is-halo; and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; R₄ is —H; R₈ is—H; and R₉ is —CH₃.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; R₄ is —H; R₈ is—CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; R₄ is —H; R₈ is—H; and R₉ is —CF₃.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; R₄ is —H; R₈ is—CF₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; R₄ is —H; R₈ is—H; and R₉ is —OCH₂CH₃.

In another embodiment, n, p, and m are 0; R₁ is —CF₃; R₄ is —H; R₈ is—OCH₂CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; R₄ is—H; R₈ is -tert-butyl; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl; R₄ is —H; R₈ is-tert-butyl; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; R₄ is—H; R₈ is —H; and R₉ is -tert-butyl.

In another embodiment, n, p, and m are 0; R₁ is —Cl; R₄ is —H; R₈ is —H;and R₉ is -tert-butyl.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; R₄ is —H; R₈ is-tert-butyl; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; R₄ is —H; R₈ is—H; and R₉ is -tert-butyl.

In another embodiment, n, p, and m are 0; R₁ is —CH₃; R₄ is —H; R₈ is—CH₃; and R₉ is —CH₃.

In another embodiment, n is 0, Ar₁ is -2-(3-chloropyridyl)-, m is 1, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group, the carbon atom to which the R₃group is attached has the R configuration, R₁₀ is —H, R₈ is methyl, andR₉ is iso-propyl.

In another embodiment, n is 0, Ar₁ is -2-(3-chloropyridyl)-, m is 1, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group, the carbon atom to which the R₃group is attached has the R configuration, R₁₀ is —H, R₈ is iso-propyl,and R₉ is methyl.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; R₄is —H; R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzoimidazole group; and R₈ and R₉ are —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; R₄ is —H; R₃ is—CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group; and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; R₄is —H; R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzoimidazole group; R₈ is —H; and R₉ is-halo. In another embodiment R₉ is —Cl. In another embodiment, R₉ is—Br. In another embodiment, R₉ is —F. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; R₄ is —H; R₃ is—CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group; R₈ is —H; and R₉ is -halo. Inanother embodiment R₉ is —Cl. In another embodiment, R₉ is —Br. Inanother embodiment, R₉ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; R₄is —H; R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzoimidazole group; R₈ is -halo; and R₉ is—H. In another embodiment R₈ is —Cl. In another embodiment, R₈ is —Br.In another embodiment, R₈ is —F. In another embodiment, the carbon atomto which the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; R₄ is —H; R₃ is—CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group; R₈ is -halo; and R₉ is —H. Inanother embodiment R₈ is —Cl. In another embodiment, R₈ is —Br. Inanother embodiment, R₈ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; R₄is —H; R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzoimidazole group; R₈ is —H; and R₉ is —CH₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; R₄ is —H; R₃ is—CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group; R₈ is —H; and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; R₄is —H; R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzoimidazole group; R₈ is —CH₃; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl,;R₄ is —H; R₃ is—CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group; R₈ is —CH₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; R₄is —H; R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzoimidazole group; R₈ is —H; and R₉ is —CF₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; R₄ is —H; R₃ is—CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group; R₈ is —H; and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; R₄is —H; R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzoimidazole group; R₈ is —CF₃; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; R₄ is —H; R₃ is—CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group; R₈ is —CF₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; R₄is —H; R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the -benzoimidazole group; R₈ is —H; and R₉ is—OCH₂CH₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; R₄ is —H; R₃ is—CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the -benzoimidazole group; R₈ is —H; and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; R₄is —H; R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzoimidazole group; R₈ is —OCH₂CH₃; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; R₄ is —H; R₃ is—CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group; R₈ is —OCH₂CH₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group, and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group, R₈ is —H, and R₉ is -halo. Inanother embodiment R₉ is —Cl. In another embodiment, R₉ is —Br. Inanother embodiment, R₉ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group, R₈ is -halo, and R₉ is —H. Inanother embodiment R₈ is —Cl. In another embodiment, R₈ is —Br. Inanother embodiment, R₈ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group, R₈ is —H, and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group, R₈ is —CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group, R₈ is —H, and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group, R₈ is —CF₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group, R₈ is —H, and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group, R₈ is —OCH₂CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group, and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group, R₈ is —H, and R₉ is -halo. Inanother embodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. Inanother embodiment, R₉ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group, R₈ is -halo, and R₉ is —H. Inanother embodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. Inanother embodiment, R₈ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group, R₈ is —H, and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group, R₈ is —CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group, R₈ is —H, and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group, R₈ is —CF₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group, R₈ is —H, and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group, R₈ is —OCH₂CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group; R₄ is —H; R₈ is -tert-butyl; andR₉ is —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —Cl, R₃ is —CH₃ andis attached to the carbon atom adjacent to the nitrogen attached to thebenzoimidazole group, R₄ is —H, R₈ is -tert-butyl, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazole group; R₄ is —H; R₈ is —H; and R₉ is-tert-butyl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —Cl, R₃ is —CH₃ andis attached to the carbon atom adjacent to the nitrogen attached to thebenzoimidazole group, R₄ is —H, R₈ is —H, and R₉ is -tert-butyl. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, R₃ is —CH₃ andis attached to the carbon atom adjacent to the nitrogen attached to thebenzoimidazole group, R₄ is —H, R₈ is -tert-butyl, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, R₃ is —CH₃ andis attached to the carbon atom adjacent to the nitrogen attached to thebenzoimidazole group, R₄ is —H, R₈ is —H, and R₉ is -tert-butyl. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, R₃ is —CH₃ andis attached to the carbon atom adjacent to the nitrogen attached to thebenzoimidazole group, R₄ is —H, R₈ is —CH₃, and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group; n is 0; m is 1; R₁ is—CH₃, —Cl, —Br, or —I; R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the benzoimidazolyl group; R₄ is—H; R₈ is —H; and R₉ is -halo. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyridyl group n is 0, m is 1, R₁ is—CH₃, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzoimidazolyl group, R₄ is —H, R₈ is —H, andR₉ is —Cl. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group; n is 0; m is 1; R₁ is—Cl, —Br, or —I; R₃ is —CH₃ and is attached to the carbon atom adjacentto the nitrogen attached to the benzoimidazolyl group; R₄ is —H; R₈ is—H; and R₉ is —Br. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0, m is 1, R₉ is—Cl, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzoimidazolyl group, R₄ is —H, R₈ is —H, andR₉ is —Br. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0, m is 1, R₁ is—CH₃, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzoimidazolyl group, R₄ is —H, R₈ is —H, andR₉ is —F. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group; p is 0; m is 1; R₁ is—CH₃, —Cl, —Br, or —I; R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the benzimidazolyl group; R₄ is —H;R₈ is —H; and R₉ is -halo. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0, m is 1, R₁ is—CH₃, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzimidazolyl group, R₄ is —H, R₁ is —H, andR₉ is —Cl. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group; p is 0; m is 1; R₁ is—Cl, —Br, or —I; R₃ is —CH₃ and is attached to the carbon atom adjacentto the nitrogen attached to the benzimidazolyl group; R₄ is —H; R₈ is—H; and R₉ is —Br. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0, m is 1, R₁ is—Cl, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzimidazolyl group, R₄ is —H, R₈ is —H, andR₉ is —Br. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0, m is 1, R₁ is—CH₃, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzimidazolyl group, R₄ is —H, R₈ is —H, andR₉ is —F. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrazinyl group; p is 0; m is 1; R₁ is—CH₃, —Cl, —Br, or —I; R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the benzimidazolyl group; R₄ is —H;R₈ is —H; and R₉ is -halo. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyrazinyl group, p is 0, m is 1, R₁ is—CH₃, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzimidazolyl group, R₄ is —H, R₈ is —H, andR₉ is —Cl. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrazinyl group; p is 0; m is 1; R₁ is—Cl, —Br, or —I; R₃ is —CH₃ and is attached to the carbon atom adjacentto the nitrogen attached to the benzimidazolyl group; R₄ is —H; R₈ is—H; and R₉ is —Br. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrazinyl group, p is 0, m is 1, R₁ is—Cl, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzimidazolyl group, R₄ is —H, R₁ is —H, andR₉ is —Br. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrazinyl group, p is 0, m is 1, R₁ is—CH₃, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzimidazolyl group, R₄ is —H, R₈ is —H, andR₉ is —F. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the benzoimidazolylgroup. In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and isattached to the carbon atom adjacent to the nitrogen attached to thebenzoimidazolyl group and the carbon to which the R₃ group is attachedis in the R configuration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the benzoimidazolylgroup. In another embodiment, m is 1 and R₃ is —CH₃ and is attached tothe carbon atom adjacent to the nitrogen attached to the benzoimidazolylgroup and the carbon to which the R₃ group is attached is in the Rconfiguration.

In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the benzoimidazolylgroup. In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and isattached to the carbon atom adjacent to the nitrogen attached to thebenzoimidazolyl group and the carbon to which the R₃ group is attachedis in the S configuration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the benzoimidazolylgroup. In another embodiment, m is 1 and R₃ is —CH₃ and is attached tothe carbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— orthe benzothiazolyl group and the carbon to which the R₃ group isattached is in the S configuration.

In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the pyridyl group,pyrimidinyl group, or pyrazinyl group. In another embodiment, m is 1 andR₃ is —(C₁-C₄)alkyl and is attached to the carbon atom adjacent to thenitrogen attached to the pyridyl group, pyrimidinyl group, or pyrazinylgroup and the carbon to which the R₃ group is attached is in the Rconfiguration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the pyridyl group,pyrimidinyl group, or pyrazinyl group. In another embodiment, m is 1 andR₃ is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the pyridyl group, pyrimidinyl group, or pyrazinyl group andthe carbon to which the R₃ group is attached is in the R configuration.

In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the pyridyl group,pyrimidinyl group, or pyrazinyl group. In another embodiment, m is 1 andR₃ is —(C₁-C₄)alkyl and is attached to the carbon atom adjacent to thenitrogen attached to the pyridyl group, pyrimidinyl group, or pyrazinylgroup and the carbon to which the R₃ group is attached is in the Sconfiguration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the pyridyl group,pyrimidinyl group, or pyrazinyl group. In another embodiment, m is 1 andR₃ is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the pyridyl group, pyrimidinyl group, or pyrazinyl group andthe carbon to which the R₃ group is attached is in the S configuration.

4.4 The Compounds of Formula (IIb)

The present invention also encompasses compounds of formula (IIb):

and pharmaceutically acceptable salts thereof, where Ar₁, R₃, R₈, R₉ ,A, x, and m, are defined above for the Benzoazolylpiperazine Compoundsof formula (IIb).

In one embodiment, Ar₁ is a pyridazinyl group.

In another embodiment, Ar₁ is a thiazanyl group.

In another embodiment, x is 1 and A is —C(O)—N(R₄)—.

In another embodiment, x is 1 and A is —C(S)—N(R₄)—.

In another embodiment x is 0.

In another embodiment, x is 1.

In another embodiment p is 0.

In another embodiment, p is 1.

In another embodiment m is 0.

In another embodiment, m is 1.

In another embodiment, R₄ is —H.

In another embodiment, R₄ is —(C₁-C₆)alkyl.

In another embodiment, R₁₀ is —H.

In another embodiment, R₁₀ is —(C₁-C₄)alkyl.

In another embodiment, R₁₀ is —CH₃.

In another embodiment, Ar₁ is a pyrazinyl group, x is 1, and A is—C(O)N(R₄)—.

In another embodiment, Ar₁ is a pyrazinyl group, x is 1, and A is—C(S)N(R₄)—.

In another embodiment, Ar₁ is a thiazanyl group, x is 1, and A is—C(O)N(R₄)—.

In another embodiment, Ar₁ is a thiazanyl group, x is 1, and A is—C(S)N(R₄)—.

In another embodiment, R₁ is —H.

In another embodiment, R₁ is —Cl.

In another embodiment, R₁ is —Br.

In another embodiment, R₁ is —I.

In another embodiment, R₁ is —F.

In another embodiment, R₁ is —(C₁-C₆)alkyl.

In another embodiment, R₁ is —CH₃.

In another embodiment, R₁ is —NO₂.

In another embodiment, R₁ is —CN.

In another embodiment, R₁ is —OH.

In another embodiment, R₁ is —OCH₃.

In another embodiment, R₁ is —NH₂.

In another embodiment, R₁ is —C(halo)₃.

In another embodiment, R₁ is —CH(halo)₂.

In another embodiment, R₁ is —CH₂(halo).

In another embodiment, p is 1 and R₂ is -halo, —CN, —OH, —O(C₁-C₆)alkyl,—NO₂, or —NH₂.

In another embodiment, p is 1 and R₂ is —(C₁-C₁₀)alkyl,—(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl,—(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,—(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, eachof which is unsubstituted or substituted with one or more R₅ groups.

In another embodiment, p is 1 and R₂ is -phenyl, -naphthyl, —(C₁₄)aryl,or -(5- to 10-membered)heteroaryl, each of which is unsubstituted orsubstituted with one or more R₆ groups;

In another embodiment, m is 1 and R₃ is -halo, —CN, —OH, —O(C₁-C₆)alkyl,—NO₂, or —NH₂.

In another embodiment, m is 1 and R₃ is —(C₁-C₁₀)alkyl,—(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl,—(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,—(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, eachof which is unsubstituted or substituted with one or more R₅ groups.

In another embodiment, m is 1 and R₃ is -phenyl, -naphthyl, -—C₁₄)arylor -(5- to 10-membered)heteroaryl, each of which is unsubstituted orsubstituted with one or more R₆ groups.

In another embodiment, R₈ and R₉ are each independently —H, halo,—(C₁-C₆)alkyl, —O(C₁-C₆)alkyl, —C(halo)₃, —CH(halo)₂, or —CH₂(halo).

In another embodiment, at least one of R₈ or R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, and R₈ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, and R₈ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -halo. In anotherembodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. In anotherembodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -halo. In anotherembodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. In anotherembodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -halo, and R₉ is —H. In anotherembodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. In anotherembodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -halo, and R₉ is —H. In anotherembodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. In anotherembodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, and R₈ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -halo. In anotherembodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. In anotherembodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -halo, and R₉ is —H. In anotherembodiment, R₈ is —Cl. In another embodiment, R₁ is —Br. In anotherembodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, and R₈ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -halo. In anotherembodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. In anotherembodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -halo, and R₉ is —H. In anotherembodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. In anotherembodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -tert-butyl, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -tert-butyl, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -tert-butyl.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -tert-butyl.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -tert-butyl, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -tert-butyl.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CH₃, and R₉ is —CH₃.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, and R₈ andR₉ are —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, and R₈ andR₉ are —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is-halo, and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is-halo, and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CH₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CH₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CF₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CF₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CF₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CF₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —OCH₂CH₃. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —OCH₂CH₃. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is—OCH₂CH₃, and R₉ is —H. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is—OCH₂CH₃, and R₉ is —H. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, and R₈ andR₉ are —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is-halo, and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CH₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CF₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CF₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —OCH₂CH₃. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is—OCH₂CH₃, and R₉ is —H. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, and R₈ andR₉ are —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is-halo, and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₁ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CH₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CF₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CF₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —OCH₂CH₃. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is—OCH₂CH₃, and R₉ is —H. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group, R₄ is —H, R₈ is-tert-butyl, and R₉ is —H. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group, R₄ is —H, R₈ is-tert-butyl, and R₉ is —H. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group, R₄ is —H, R₈ is —H, andR₉ is -tert-butyl. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group, R₄ is —H, R₈ is —H, andR₉ is -tert-butyl. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group, R₄ is —H, R₈ is-tert-butyl, and R₉ is —H. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group, R₄ is —H, R₈ is —H, andR₉ is -tert-butyl. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group, R₄ is —H, R₈ is —CH₃,and R₉ is —CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, andR₈ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, andR₉ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is —H, and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—H, and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is -halo, and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is-halo, and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is —H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is —CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is —H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is —CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is —H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is —OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, andR₈ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —H, and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is -halo, and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, andR₈ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is —H, and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is -halo, and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is —H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is —CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is —H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is —CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is —H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is —OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is -tert-butyl, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is-tert-butyl, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is —H, and R₉ is -tert-butyl.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—H, and R₉ is -tert-butyl.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is -tert-butyl, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —H, and R₉ is -tert-butyl.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —CH₃, and R₉ is —CH₃.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —H, and R₉ is -halo. Inanother embodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. Inanother embodiment, R₉ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —H, and R₉ is -halo. Inanother embodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. Inanother embodiment, R₉ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is -halo, and R₉ is —H. Inanother embodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. Inanother embodiment, R₈ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is -halo, and R₉ is —H. Inanother embodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. Inanother embodiment, R₈ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —H, and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —H, and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —H, and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —H, and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —CF₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —CF₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —H, and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —H, and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —OCH₂CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —OCH₂CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —H, and R₉ is -halo. Inanother embodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. Inanother embodiment, R₉ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is -halo, and R₉ is —H. Inanother embodiment, R₈ is —Cl. In another embodiment, R₉ is —Br. Inanother embodiment, R₈ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —H, and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₁ is —H, and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —CF₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —H, and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —OCH₂CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —H, and R₉ is -halo. Inanother embodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. Inanother embodiment, R₉ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is -halo, and R₉ is —H. Inanother embodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. Inanother embodiment, R₈ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —H, and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —H, and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —CF₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —H, and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzoimidazolyl group, R₈ is —OCH₂CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₃ is —CH₃and is attached to the carbon atom adjacent to the nitrogen attached tothe benzoimidazolyl group, R₄ is —H, R₈ is -tert-butyl, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₃ is —CH₃ andis attached to the carbon atom adjacent to the nitrogen attached to thebenzoimidazolyl group, R₄ is —H, R₈ is -tert-butyl, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₃ is —CH₃and is attached to the carbon atom adjacent to the nitrogen attached tothe benzoimidazolyl group, R₄ is —H, R₈ is —H, and R₉ is -tert-butyl. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₃ is —CH₃ andis attached to the carbon atom adjacent to the nitrogen attached to thebenzoimidazolyl group, R₄ is —H, R₈ is —H, and R₉ is -tert-butyl. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₃ is —CH₃and is attached to the carbon atom adjacent to the nitrogen attached tothe benzoimidazolyl group, R₄ is —H, R₈ is -tert-butyl, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₃ is —CH₃and is attached to the carbon atom adjacent to the nitrogen attached tothe benzoimidazolyl group, R₄ is —H, R₈ is —H, and R₉ is -tert-butyl. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₃ is —CH₃and is attached to the carbon atom adjacent to the nitrogen attached tothe benzoimidazolyl group, R₄ is —H, R₈ is —CH₃, and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—CH₃ or -halo, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached tothe carbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)—group, R₄ is —H, R₈ is —H, and R₉ is -halo. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.In another embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —Cl. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is-halo, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —Br. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—Cl, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbonatom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₄ is—H, R₈ is —H, and R₉ is —Br. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —F. In another embodiment, the carbon atomto which the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—CH₃ or -halo, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached tothe carbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)—group, R₄ is —H, R₈ is —H, and R₉ is -halo. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.In another embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —Cl. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is-halo, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —Br. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—Cl, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbonatom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₄ is—H, R₈ is —H, and R₉ is —Br. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —F. In another embodiment, the carbon atomto which the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—CH₃ or -halo, x is 0, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the benzoimidazolyl group, R₄ is—H, R₈ is —H, and R₉ is -halo. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzoimidazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Cl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is-halo, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzoimidazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Br. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—Cl, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzoimidazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Br. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzoimidazolyl group, R₄ is —H, R₈ is —H,and R₉ is —F. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—CH₃ or -halo, x is 0, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the benzoimidazolyl group, R₄ is—H, R₈ is —H, and R₉ is -halo. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzoimidazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Cl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is-halo, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzoimidazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Br. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—Cl, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzoimidazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Br. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzoimidazolyl group, R₄ is —H, R₈ is —H,and R₉ is —F. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)—when x is 1 or the benzoimidazolyl group when x is 0. In anotherembodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached to the carbonatom adjacent to the nitrogen attached to the —C(O)—N(R₄)— when x is 1or the benzoimidazolyl group when x is 0 and the carbon to which the R₃group is attached is in the R configuration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— when xis 1 or the benzoimidazolyl group when x is 0. In another embodiment, mis 1 and R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the —C(O)—N(R₄)— when x is 1 or the benzoimidazolylgroup when x is 0 and the carbon to which the R₃ group is attached is inthe R configuration.

In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)—when x is 1 or the benzoimidazolyl group when x is 0. In anotherembodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached to the carbonatom adjacent to the nitrogen attached to the —C(O)—N(R₄)— when x is 1or the benzoimidazolyl group when x is 0 and the carbon to which the R₃group is attached is in the S configuration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— when xis 1 or the benzoimidazolyl group when x is 0. In another embodiment, mis 1 and R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the —C(O)—N(R₄)— when x is 1 or the benzoimidazolylgroup when x is 0 and the carbon to which the R₃ group is attached is inthe S configuration.

In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the pyridazinylgroup or thiazanyl group. In another embodiment, m is 1 and R₃ is—(C₁-C₄)alkyl and is attached to the carbon atom adjacent to thenitrogen attached to the pyridazinyl group or thiazanyl group and thecarbon to which the R₃ group is attached is in the R configuration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the pyridazinyl groupor thiazanyl group. In another embodiment, m is 1 and R₃ is —CH₃ and isattached to the carbon atom adjacent to the nitrogen attached to thepyridazinyl group or thiazanyl group and the carbon to which the R₃group is attached is in the R configuration.

In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the pyridazinylgroup or thiazanyl group. In another embodiment, m is 1 and R₃ is—(C₁-C₄)alkyl and is attached to the carbon atom adjacent to thenitrogen attached to the pyridazinyl group or thiazanyl group and thecarbon to which the R₃ group is attached is in the S configuration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the pyridazinyl groupor thiazanyl group. In another embodiment, m is 1 and R₃ is —CH₃ and isattached to the carbon atom adjacent to the nitrogen attached to thepyridazinyl group or thiazanyl group and the carbon to which the R₃group is attached is in the S configuration.

4.5 The Compounds of Formula (IIIa)

The present invention encompasses compounds of Formula (IIIa)

and pharmaceutically acceptable salts thereof, where Ar₁, R₃, R₈, R₉, A,x, and m, are defined above for the Benzoazolylpiperazine Compounds offormula (IIIa).

In one embodiment, Ar₁ is a pyridyl group.

In another embodiment, Ar₁ is a pyrimidinyl group.

In another embodiment, x is 1 and A is —C(O)—N(R₄)—.

In another embodiment, x is 1 and A is —C(S)—N(R₄)—.

In another embodiment x is 0.

In another embodiment x is 1.

In another embodiment n or p is 0.

In another embodiment n or p is 1.

In another embodiment m is 0.

In another embodiment m is 1.

In another embodiment, Ar₁ is a pyridyl group, x is 1, and A is—C(O)N(R₄)—.

In another embodiment, Ar₁ is a pyridyl group, x is 1, and A is—C(S)N(R₄)—.

In another embodiment, Ar₁ is a pyrimidinyl group, x is 1, and A is—C(O)N(R₄)—.

In another embodiment, Ar₁ is a pyrimidinyl group, x is 1, and A is—C(S)N(R₄)—.

In another embodiment, R₁ is —Cl.

In another embodiment, R₁ is —Br.

In another embodiment, R₁ is —I.

In another embodiment, R₁ is —(C₁-C₆)alkyl.

In another embodiment, R₁ is —CH₃.

In another embodiment, R₁ is —NO₂.

In another embodiment, R₁ is —CN.

In another embodiment, R₁ is —OH.

In another embodiment, R₁ is —OCH₃.

In another embodiment, R₁ is —NH₂.

In another embodiment, R₁ is —C(halo)₃.

In another embodiment, R₁ is —CH(halo)₂.

In another embodiment, R₁ is —CH₂(halo).

In another embodiment, n and p are 1 and R₂ is -halo, —CN, —OH,—O(C₁-C₆)alkyl, —NO₂, or —NH₂.

In another embodiment, n and p are 1 and R₂ is —(C₁-C₁₀)alkyl,—(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl,—(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,—(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, eachof which is unsubstituted or substituted with one or more R₅ groups.

In another embodiment, n and p are 1 and R₂ is -phenyl, -naphthyl,—(C₁₄)aryl, or -(5- to 10-membered)heteroaryl, each of which isunsubstituted or substituted with one or more R₆ groups;

In another embodiment, m is 1 and R₃ is -halo, —CN, —OH, —O(C₁-C₆)alkyl,—NO₂, or —NH₂.

In another embodiment, m is 1 and R₃ is —(C₁-C₁₀)alkyl,—(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl,—(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,—(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, eachof which is unsubstituted or substituted with one or more R₅ groups.

In another embodiment, m is 1 and R₃ is -phenyl, -naphthyl, —(C₁₄)arylor -(5- to 10-membered)heteroaryl, each of which is unsubstituted orsubstituted with one or more R₆ groups.

In another embodiment, R₄ is —H.

In another embodiment, R₄ is —(C₁-C₆)alkyl.

In another embodiment, R₈ and R₉ are each independently —H, halo,—(C₁-C₆)alkyl, —O(C₁-C₆)alkyl, —C(halo)₃, —CH(halo)₂, or —CH₂(halo).

In another embodiment, at least one of R₈ or R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 1;A is —C(O)—N(R₄)—; R₄ is —H; and R₈ and R₉ are —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; and R₈ and R₉ are —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 1;A is —C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is -halo. In anotherembodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. In anotherembodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is -halo. In anotherembodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. In anotherembodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 1;A is —C(O)—N(R₄)—; R₄ is —H; R₈ is -halo; and R₉ is —H. In anotherembodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. In anotherembodiment, R₈ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is -halo; and R₉ is —H. In anotherembodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. In anotherembodiment, R₈ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 1;A is —C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is —CH₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is —CH₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 1;A is —C(O)—N(R₄)—; R₄ is —H; R₈ is —CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 1;A is —C(O)—N(R₄)—; R₄ is —H, R₈ is —H; and R₉ is —CF₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is —CF₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 1;A is —C(O)—N(R₄)—; R₄ is —H; R₈ is —CF₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₁ is —CF₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 1;A is —C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is —OCH₂CH₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is —OCH₂CH₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 1;A is —C(O)—N(R₄)—; R₄ is —H; R₈ is —OCH₂CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —OCH₂CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, and R₈ and R₉ are —H.

In another embodiment, n, p, and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₁ is —H, and R₉ is -halo. In anotherembodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. In anotherembodiment, R₉ is —F.

In another embodiment, n, p, and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -halo, and R₉ is —H. In anotherembodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. In anotherembodiment, R₈ is —F.

In another embodiment, n, p, and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CH₃.

In another embodiment, n, p, and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CH₃, and R₉ is —H.

In another embodiment, n, p, and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CF₃.

In another embodiment, n, p, and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CF₃, and R₉ is —H.

In another embodiment, n, p, and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —OCH₂CH₃.

In another embodiment, n, p, and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —OCH₂CH₃, and R₉ is —H.

In another embodiment, n, p, and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, and R₈ and R₉ are —H.

In another embodiment, n, p, and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -halo. In anotherembodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. In anotherembodiment, R₉ is —F.

In another embodiment, n, p, and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -halo, and R₉ is —H. In anotherembodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. In anotherembodiment, R₈ is —F.

In another embodiment, n, p, and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CH₃.

In another embodiment, n, p, and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H. R₈ is —CH₃, and R₉ is —H.

In another embodiment, n, p, and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CF₃.

In another embodiment, n, p, and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CF₃, and R₉ is —H.

In another embodiment, n, p, and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —OCH₂CH₃.

In another embodiment, n, p, and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —OCH₂CH₃, and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 1;A is —C(O)—N(R₄)—; R₄ is —H; R₈ is -tert-butyl; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is -tert-butyl; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 1;A is —C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is -tert-butyl.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is -tert-butyl.

In another embodiment, n, p, and m are 0; R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -tert-butyl, and R₉ is —H.

In another embodiment, n, p, and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -tert-butyl.

In another embodiment, n, p, and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CH₃, and R₉ is —CH₃.

In another embodiment, n is 0, Ar₁ is -2-(3-nitropyridyl)-, m is 0, x is0, and R₈ and R₉ are —H.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 1; A is —C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group;and R₈ and R₉ are —H. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0; m is 1, R₁ is —Cl; x is 1, A is—C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group; and R₈ andR₉ are —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 1; A is —C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group;R₈ is —H; and R₉ is -halo. In another embodiment R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group; R₈ is —H;and R₉ is -halo. In another embodiment R₉ is —Cl. In another embodiment,R₉ is —Br. In another embodiment, R₉ is —F. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.In another embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 1; A is —C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group;R₈ is -halo; and R₉ is —H. In another embodiment R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group; R₈ is-halo; and R₉ is —H. In another embodiment R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 1; A is —C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group;R₈ is —H; and R₉ is —CH₃. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group; R₈ is —H;and R₉ is —CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 1; A is —C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group;R₈ is —CH₃; and R₉ is —H. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group; R₈ is —CH₃;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 1; A is —C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group;R₈ is —H; and R₉ is —CF₃. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group; R₈ is —H;and R₉ is —CF₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 1; A is —C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group;R₈ is —CF₃; and R₉ is —H. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group; R₈ is —CF₃;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 1; A is —C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group;R₈ is —H; and R₉ is —OCH₂CH₃. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group; R₈ is —H;and R₉ is —OCH₂CH₃. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 1; A is —C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group;R₈ is —OCH₂CH₃; and R₉ is —H. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group; R₈ is—OCH₂CH₃; and R₉ is —H. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, and R₈ andR₉ are —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is -halo. In another embodiment R₉ is —Cl. In another embodiment,R₉ is —Br. In another embodiment, R₉ is —F. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.In another embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is-halo, and R₉ is —H. In another embodiment R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₁ is —H,and R₉ is —CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CH₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CF₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CF₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —OCH₂CH₃. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is—OCH₂CH₃, and R₉ is —H. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, and R₈ andR₉ are —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is -halo. In another embodiment R₉ is —Cl. In another embodiment,R₉ is —Br. In another embodiment, R₉ is —F. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.In another embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is-halo, and R₉ is —H. In another embodiment R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CH₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CF₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CF₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —OCH₂CH₃. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is—OCH₂CH₃, and R₉ is —H. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 1; A is —C(O)—N(R₄)—; R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group; R₄ is —H;R₈ is -tert-butyl; and R₉ is —H. In another embodiment, the carbon atomto which the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group; R₄ is —H; R₈ is-tert-butyl; and R₉ is —H. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 1; A is —C(O)—N(R₄)—; R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group; R₄ is —H;R₈ is —H; and R₉ is -tert-butyl. In another embodiment, the carbon atomto which the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; x is 1; A is—C(O)—N(R₄)—; R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group; R₄ is —H; R₈ is —H; andR₉ is -tert-butyl. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group, R₄ is —H, R₈ is-tert-butyl, and R₉ is —H. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group, R₄ is —H, R₈ is —H, andR₉ is -tert-butyl. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group, R₄ is —H, R₈ is —CH₃,and R₉ is —CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 0;R₄ is —H; and R₈ and R₉ are —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 0; R₄ is —H;and R₈ and R₉ are —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 0;R₄ is —H; R₈ is —H; and R₉ is -halo. In another embodiment, R₉ is —Cl.In another embodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 0; R₄ is —H;R₈ is —H; and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 0;R₄ is —H; R₈ is -halo; and R₉ is —H. In another embodiment, R₈ is —Cl.In another embodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl, x is 0; R₄ is —H;R₈ is -halo; and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 0;R₄ is —H; R₈ is —H; and R₉ is —CH₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 0; R₄ is —H;R₈ is —H; and R₉ is —CH₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 0;R₄ is —H; R₈ is —CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 0; R₄ is —H;R₈ is —CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 0;R₄ is —H; R₈ is —H; and R₉ is —CF₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 0; R₄ is —H;R₈ is —H; and R₉ is —CF₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 0;R₄ is —H; R₈ is —CF₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 0; R₄ is —H;R₈ is —CF₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 0;R₄ is —H; R₈ is —H; and R₉ is —OCH₂CH₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 0; R₄ is —H;R₈ is —H; and R₉ is —OCH₂CH₃.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 0;R₄ is —H; R₈ is —OCH₂CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 0; R₄ is —H;R₈ is —OCH₂CH₃; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —CH₃, x is 0; R₄ is —H,and R₈ and R₉ are —H.

In another embodiment, n, p, and m are 0; R₁ is —CH₃, x is 0; R₄ is —H,R₈ is —H, and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0; R₁ is —CH₃, x is 0; R₄ is —H,R₈ is -halo, and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, n, p, and m are 0; R₁ is —CH₃, x is 0; R₄ is —H,R₈ is —H, and R₉ is —CH₃.

In another embodiment, n, p, and m are 0, R₁ is —CH₃, x is 0, R₄ is —H,R₈ is —CH₃, and R₉ is —H.

In another embodiment, n, p, and m are 0, R₁ is —CH₃, x is 0, R₄ is —H,R₈ is —H, and R₉ is —CF₃.

In another embodiment, n, p, and m are 0, R₁ is —CH₃, x is 0, R₄ is —H,R₈ is —CF₃, and R₉ is —H.

In another embodiment, n, p, and m are 0, R₁ is —CH₃, x is 0, R₄ is —H,R₈ is —H, and R₉ is —OCH₂CH₃.

In another embodiment, n, p, and m are 0, R₁ is —CH₃, x is 0, R₄ is —H,R₈ is —OCH₂CH₃, and R₉ is —H.

In another embodiment, n, p, and m are 0, R₁ is —CF₃, x is 0, R₄ is —H,and R₈ and R₉ are —H.

In another embodiment, n, p, and m are 0, R₁ is —CF₃, x is 0, R₄ is —H,R₈ is —H, and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, n, p, and m are 0, R₁ is —CF₃, x is 0, R₄ is —H,R₈ is -halo, and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, n, p, and m are 0, R₁ is —CF₃, x is 0, R₄ is —H,R₈ is —H, and R₉ is —CH₃.

In another embodiment, n, p, and m are 0, R₁ is —CF₃, x is 0, R₄ is —H,R₈ is —CH₃, and R₉ is —H.

In another embodiment, n, p, and m are 0, R₁ is —CF₃, x is 0, R₄ is —H,R₈ is —H, and R₉ is —CF₃.

In another embodiment, n, p, and m are 0, R₁ is —CF₃, x is 0, R₄ is —H,R₈ is —CF₃, and R₉ is —H.

In another embodiment, n, p, and m are 0, R₁ is —CF₃, x is 0, R₄ is —H,R₈ is —H, and R₉ is —OCH₂CH₃.

In another embodiment, n, p, and m are 0, R₁ is —CF₃, x is 0, R₄ is —H,R₈ is —OCH₂CH₃, and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 0;R₄ is —H; R₈ is -tert-butyl; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 0; R₄ is —H;R₈ is -tert-butyl; and R₉ is —H.

In another embodiment, n, p, and m are 0; R₁ is —Cl, —Br, or —I; x is 0;R₄ is —H; R₈ is —H; and R₉ is -tert-butyl.

In another embodiment, n, p, and m are 0; R₁ is —Cl; x is 0; R₄ is —H;R₈ is —H; and R₉ is -tert-butyl.

In another embodiment, n, p, and m are 0, R₁ is —CH₃, x is 0, R₄ is —H,R₈ is -tert-butyl, and R₉ is —H.

In another embodiment, n, p, and m are 0, R₁ is —CH₃, x is 0, R₄ is —H,R₈ is —H, and R₉ is -tert-butyl.

In another embodiment, n, p, and m are 0, R₁ is —CH₃, x is 0, R₄ is —H,R₈ is —CH₃, and R₉ is —CH₃.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 0; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atom adjacentto the nitrogen attached to the benzooxazolyl group; and R₈ and R₉ are—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1, R₁ is —Cl; x is 0; R₄ is—H; R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group, and R₈ and R₉ are —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 0; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atom adjacentto the nitrogen attached to the benzooxazolyl group; R₈ is —H; and R₉ is-halo. In another embodiment R₉ is —Cl. In another embodiment, R₉ is—Br. In another embodiment, R₉ is —F. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; x is 0; R₄ is—H; R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group; R₈ is —H; and R₉ is -halo.In another embodiment R₉ is —Cl. In another embodiment, R₉ is —Br. Inanother embodiment, R₉ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 0; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atom adjacentto the nitrogen attached to the benzooxazolyl group; R₈ is -halo; and R₉is —H. In another embodiment R₈ is —Cl. In another embodiment, R₈ is—Br. In another embodiment, R₈ is —F. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, n and p are 0; m is 1, R₁ is —Cl; x is 0; R₄ is—H; R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group; R₈ is -halo; and R₉ is —H.In another embodiment R₈ is —Cl. In another embodiment, R₈ is —Br. Inanother embodiment, R₈ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 0; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atom adjacentto the nitrogen attached to the benzooxazolyl group; R₈ is —H; and R₉ is—CH₃. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1, R₁ is —Cl; x is 0; R₄ is—H; R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group; R₈ is —H; and R₉ is —CH₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 0; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atom adjacentto the nitrogen attached to the benzooxazolyl group; R₈ is —CH₃, and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; x is 0; R₄ is—H; R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group; R₈ is —CH₃; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 0; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atom adjacentto the nitrogen attached to the benzooxazolyl group; R₈ is —H; and R₉ is—CF₃. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, n and p 0; m is 1; R₁ is —Cl; x is 0; R₄ is —H;R₃ is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group; R₈ is —H; and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 0; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atom adjacentto the nitrogen attached to the benzooxazolyl group; R₈ is —CF₃; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; x is 0; R₄ is—H; R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group; R₈ is —CF₃; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 0; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atom adjacentto the nitrogen attached to the benzooxazolyl group; R₈ is —H; and R₉ is—OCH₂CH₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; x is 0; R₄ is—H; R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group; R₈ is —H; and R₉ is—OCH₂CH₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 0; R₄ is —H; R₃ is —CH₃ and is attached to the carbon atom adjacentto the nitrogen attached to the benzooxazolyl group; R₈ is —OCH₂CH₃; andR₉ is —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; x is 0; R₄ is—H; R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group; R₈ is —OCH₂CH₃; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group, and R₈ and R₉ are —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group, R₈ is —H, and R₉ is -halo.In another embodiment R₉ is —Cl. In another embodiment, R₉ is —Br. Inanother embodiment, R₉ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group, R₈ is -halo, and R₉ is —H.In another embodiment R₈ is —Cl. In another embodiment, R₈ is —Br. Inanother embodiment, R₈ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group, R₈ is —H, and R₉ is —CH₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group, R₈ is —CH₃, and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group, R₈ is —H, and R₉ is —CF₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group, R₈ is —CF₃, and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group, R₈ is —H, and R₉ is—OCH₂CH₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group, R₈ is —OCH₂CH₃, and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group, and R₈ and R₉ are —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group, R₈ is —H, and R₉ is -halo.In another embodiment R₉ is —Cl. In another embodiment, R₉ is —Br. Inanother embodiment, R₉ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group, R₈ is -halo, and R₉ is —H.In another embodiment R₈ is —Cl. In another embodiment, R₈ is —Br. Inanother embodiment, R₈ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group, R₈ is —H, and R₉ is —CH₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group, R₈ is —CH₃, and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group, R₈ is —H, and R₉ is —CF₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group, R₈ is —CF₃, and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group, R₈ is —H, and R₉ is—OCH₂CH₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CF₃, x is 0, R₄ is—H, R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group, R₈ is —OCH₂CH₃, and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 0; R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group; R₄ is —H, R₈ is-tert-butyl, and R₉ is —H. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; x is 0; R₃ is—CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group; R₄ is —H; R₈ is -tert-butyl; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl, —Br, or —I; xis 0; R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the benzooxazolyl group; R₄ is —H; R₈ is —H; and R₉is -tert-butyl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0; m is 1; R₁ is —Cl; x is 0; R₃ is—CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group; R₄ is —H; R₈ is —H; and R₉ is-tert-butyl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 0, R₃ is—CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₄ is —H, R₈ is -tert-butyl, and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 0, R₃ is—CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₄ is —H, R₈ is —H, and R₉ is-tert-butyl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, n and p are 0, m is 1, R₁ is —CH₃, x is 0, R₃ is—CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₄ is —H, R₈ is —CH₃, and R₉ is—CH₃. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group; n is 0; m is 1; R₁ is—CH₃, —Cl, —Br, or —I; x is 1; A is —C(O)—N(R₄)—; R₃ is —CH₃ and isattached to the carbon atom adjacent to the nitrogen attached to the—C(O)—N(R₄)— group; R₄ is —H; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration.

In another embodiment, Ar₁ is a pyridyl group, n is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —Cl. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration.

In another embodiment, Ar₁ is a pyridyl group; n is 0; m is 1; R₁ is—Cl, —Br, or —I; x is 1; A is —C(O)—N(R₄)—; R₃ is —CH₃ and is attachedto the carbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)—group; R₄ is —H; R₈ is —H; and R₉ is —Br. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0, m is 1, R₁ is—Cl, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbonatom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₄ is—H, R₈ is —H, and R₉ is —Br. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —F. In another embodiment, the carbon atomto which the R₃ group is attached has the R configuration.

In another embodiment, Ar₁ is a pyrimidinyl group; p is 0; m is 1; R₁ is—CH₃, —Cl, —Br, —I; x is 1; A is —C(O)—N(R₄)—; R₃ is —CH₃ and isattached to the carbon atom adjacent to the nitrogen attached to the—C(O)—N(R₄)— group; R₄ is —H; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —Cl. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration.

In another embodiment, Ar₁ is a pyrimidinyl group; p is 0; m is 1; R₁ is—Cl, —Br, or —I; x is 1; A is —C(O)—N(R₄)—; R₃ is —CH₃ and is attachedto the carbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)—group; R₄ is —H; R₈ is —H; and R₉ is —Br. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0, m is 1, R₁ is—Cl, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbonatom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₄ is—H, R₈ is —H, and R₉ is —Br. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —F. In another embodiment, the carbon atomto which the R₃ group is attached has the R configuration.

In another embodiment, Ar₁ is a pyridyl group; n is 0; m is 1; R₁ is—CH₃, —Cl, —Br, or —I; x is 0; R₃ is —CH₃ and is attached to the carbonatom adjacent to the nitrogen attached to the benzooxazolyl group; R₄ is—H; R₈ is —H; and R₉ is -halo. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzooxazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Cl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration.

In another embodiment, Ar₁ is a pyridyl group; n is 0; m is 1; R₁ is—Cl, —Br, or —I; x is 0; R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the benzooxazolyl group; R₄ is —H;R₈ is —H; and R₉ is —Br. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0, m is 1, R₁ is—Cl, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzooxazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Br. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzooxazolyl group, R₄ is —H, R₈ is —H,and R₉ is —F. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration.

In another embodiment, Ar₁ is a pyrimidinyl group; p is 0; m is 1; R₁ is—CH₃, —Cl, —Br, or —I; x is 0; R₃ is —CH₃ and is attached to the carbonatom adjacent to the nitrogen attached to the benzooxazolyl group; R₄ is—H; R₈ is —H; and R₉ is -halo. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzooxazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Cl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration.

In another embodiment, Ar₁ is a pyrimidinyl group; p is 0; m is 1; R₁ is—Cl, —Br, or —I; x is 0; R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the benzooxazolyl group; R₄ is —H;R₈ is —H; and R₉ is —Br. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0, m is 1, R₁ is—Cl, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzooxazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Br. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzooxazolyl group, R₄ is —H, R₈ is —H,and R₉ is —F. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration.

In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— orthe benzooxazolyl group. In another embodiment, m is 1 and R₃ is—(C₁-C₄)alkyl and is attached to the carbon atom adjacent to thenitrogen attached to the —C(O)—N(R₄)— or the benzooxazolyl group and thecarbon to which the R₃ group is attached is in the R configuration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— or thebenzooxazolyl group. In another embodiment, m is 1 and R₃ is —CH₃ and isattached to the carbon atom adjacent to the nitrogen attached to the—C(O)—N(R₄)— or the benzooxazolyl group and the carbon to which the R₃group is attached is in the R configuration.

In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— orthe benzooxazolyl group. In another embodiment, m is 1 and R₃ is—(C₁-C₄)alkyl and is attached to the carbon atom adjacent to thenitrogen attached to the —C(O)—N(R₄)— or the benzooxazolyl group and thecarbon to which the R₃ group is attached is in the S configuration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— or thebenzooxazolyl group. In another embodiment, m is 1 and R₃ is —CH₃ and isattached to the carbon atom adjacent to the nitrogen attached to the—C(O)—N(R₄)— or the benzooxazolyl group and the carbon to which the R₃group is attached is in the S configuration.

In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the pyridyl groupor pyrimidinyl group. In another embodiment, m is 1 and R₃ is—(C₁-C₄)alkyl and is attached to the carbon atom adjacent to thenitrogen attached to the pyridyl group or pyrimidinyl group and thecarbon to which the R₃ group is attached is in the R configuration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the pyridyl group orpyrimidinyl group. In another embodiment, m is 1 and R₃ is —CH₃ and isattached to the carbon atom adjacent to the nitrogen attached to thepyridyl group or pyrimidinyl group and the carbon to which the R₃ groupis attached is in the R configuration.

In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the pyridyl groupor pyrimidinyl group. In another embodiment, m is 1 and R₃ is—(C₁-C₄)alkyl and is attached to the carbon atom adjacent to thenitrogen attached to the pyridyl group or pyrimidinyl group and thecarbon to which the R₃ group is attached is in the S configuration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the pyridyl group orpyrimidinyl group. In another embodiment, m is 1 and R₃ is —CH₃ and isattached to the carbon atom adjacent to the nitrogen attached to thepyridyl group or pyrimidinyl group and the carbon to which the R₃ groupis attached is in the S configuration.

4.6 The Compounds of Formula (IIIb)

The present invention also encompasses compounds of formula (IIIb):

and pharmaceutically acceptable salts thereof, where Ar₁, R₃, R₈, R₉, A,x, and m, are defined above for the Benzoazolylpiperazine Compounds offormula (IIIb).

In one embodiment, Ar₁ is a pyrazinyl group.

In another embodiment, Ar₁ is a pyridazinyl group.

In another embodiment, Ar₁ is a thiazanyl group.

In another embodiment, x is 1 and A is —C(O)—N(R₄)—.

In another embodiment, x is 1 and A is —C(S)—N(R₄)—.

In another embodiment x is 0.

In another embodiment, x is 1.

In another embodiment, p is 0.

In another embodiment, p is 1.

In another embodiment, m is 0.

In another embodiment, m is 1.

In another embodiment, Ar₁ is a pyrazinyl group, x is 1, and A is—C(O)N(R₄)—.

In another embodiment, Ar₁ is a pyrazinyl group, x is 1, and A is—C(S)N(R₄)—.

In another embodiment, Ar₁ is a pyridazinyl group, x is 1, and A is—C(O)N(R₄)—.

In another embodiment, Ar₁ is a pyridazinyl group, x is 1, and A is—C(S)N(R₄)—.

In another embodiment, Ar₁ is a thiazanyl group, x is 1, and A is—C(O)N(R₄)—.

In another embodiment, Ar₁ is a thiazanyl group, x is 1, and A is—C(S)N(R₄)—.

In another embodiment, R₁ is —H.

In another embodiment, R₁ is —Cl.

In another embodiment, R₁ is —Br.

In another embodiment, R₁ is —I.

In another embodiment, R₁ is —F.

In another embodiment, R₁ is —(C₁-C₆)alkyl.

In another embodiment, R₁ is —CH₃.

In another embodiment, R₁ is —NO₂.

In another embodiment, R₁ is —CN.

In another embodiment, R₁ is —OH.

In another embodiment, R₁ is —OCH₃.

In another embodiment, R₁ is —NH₂.

In another embodiment, R₁ is —C(halo)₃.

In another embodiment, R₁ is —CH(halo)₂.

In another embodiment, R₁ is —CH₂(halo).

In another embodiment, p is 1 and R₂ is -halo, —CN, —OH, —O(C₁-C₆)alkyl,—NO₂, or —NH₂.

In another embodiment, p is 1 and R₂ is —(C₁-C₁₀)alkyl,—(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl,—(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,—(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, eachof which is unsubstituted or substituted with one or more R₅ groups.

In another embodiment, p is 1 and R₂ is -phenyl, -naphthyl, —(C₁₄)aryl,or -(5- to 10-membered)heteroaryl, each of which is unsubstituted orsubstituted with one or more R₆ groups;

In another embodiment, m is 1 and R₃ is -halo, —CN, —OH, —O(C₁-C₆)alkyl,—NO₂, or —NH₂.

In another embodiment, m is 1 and R₃ is —(C₁-C₁₀)alkyl,—(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl,—(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,—(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, eachof which is unsubstituted or substituted with one or more R₅ groups.

In another embodiment, m is 1 and R₃ is -phenyl, -naphthyl, —(C₁₄)arylor -(5- to 10-membered)heteroaryl, each of which is unsubstituted orsubstituted with one or more R₆ groups.

In another embodiment, R₄ is —H.

In another embodiment, R₄ is —(C₁-C₆)alkyl.

In another embodiment, R₈ and R₉ are each independently —H, halo,—(C₁-C₆)alkyl, —O(C₁-C₆)alkyl, —C(halo)₃, —CH(halo)₂, or —CH₂(halo).

In another embodiment, at least one of R₈ or R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, and R₈ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, and R₈ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -halo. In anotherembodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. In anotherembodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -halo. In anotherembodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. In anotherembodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -halo, and R₉ is —H. In anotherembodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. In anotherembodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -halo, and R₉ is —H. In anotherembodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. In anotherembodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, and R₈ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -halo. In anotherembodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. In anotherembodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -halo, and R₉ is —H. In anotherembodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. In anotherembodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, and R₈ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -halo. In anotherembodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. In anotherembodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -halo, and R₉ is —H. In anotherembodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. In anotherembodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -tert-butyl, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -tert-butyl, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -tert-butyl.

In another embodiment, p and m are 0, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -tert-butyl.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is -tert-butyl, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —H, and R₉ is -tert-butyl.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₈ is —CH₃, and R₉ is —CH₃.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, and R₈ andR₉ are —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, and R₈ andR₉ are —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is-halo, and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is-halo, and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CH₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CH₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CF₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CF₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CF₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CF₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —OCH₂CH₃. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —OCH₂CH₃. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is—OCH₂CH₃, and R₉ is —H. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is—OCH₂CH₃, and R₉ is —H. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, and R₈ andR₉ are —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is -halo. In another embodiment R₉ is —Cl. In another embodiment,R₉ is —Br. In another embodiment, R₉ is —F. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.In another embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is-halo, and R₉ is —H. In another embodiment R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CH₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CF₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CF₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —OCH₂CH₃. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is—OCH₂CH₃, and R₉ is —H. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, and R₈ andR₉ are —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is -halo. In another embodiment R₉ is —Cl. In another embodiment,R₉ is —Br. In another embodiment, R₉ is —F. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.In another embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is-halo, and R₉ is —H. In another embodiment R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CH₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —CF₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —CF₃,and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₈ is —H,and R₉ is —OCH₂CH₃. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 1, A is—C(O)—N(R₄)—, R₄ is —H, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₁ is—OCH₂CH₃, and R₉ is —H. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is halo, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group, R₄ is —H, R₈ is-tert-butyl, and R₉ is —H. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group, R₄ is —H, R₈ is-tert-butyl, and R₉ is —H. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group, R₄ is —H, R₈ is —H, andR₉ is -tert-butyl. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group, R₄ is —H, R₈ is —H, andR₉ is -tert-butyl. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group, R₄ is —H, R₈ is-tert-butyl, and R₉ is —H. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group, R₄ is —H, R₈ is —H, andR₉ is -tert-butyl. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 1, A is—C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the —C(O)—N(R₄)— group, R₄ is —H, R₈ is —CH₃,and R₉ is —CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, andR₈ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, andR₈ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is —H, and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—H, and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is -halo, and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is-halo, and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is —H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is —CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is —H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is —CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₉ is -halo, x is 0, R₄ is —H, R₈is —H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is —OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, andR₈ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —H, and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is -halo, and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, andR₈ and R₉ are —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is —H, and R₉ is -halo. In another embodiment, R₉ is —Cl. In anotherembodiment, R₉ is —Br. In another embodiment, R₉ is —F.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is -halo, and R₉ is —H. In another embodiment, R₈ is —Cl. In anotherembodiment, R₈ is —Br. In another embodiment, R₈ is —F.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is —H, and R₉ is —CH₃.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is —CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is —H, and R₉ is —CF₃.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is —CF₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is —H, and R₉ is —OCH₂CH₃.

In another embodiment, p and m are 0, R₁ is —CF₃, x is 0, R₄ is —H, R₈is —OCH₂CH₃, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is -tert-butyl, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is-tert-butyl, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is -halo, x is 0, R₄ is —H, R₈is —H, and R₉ is -tert-butyl.

In another embodiment, p and m are 0, R₁ is —Cl, x is 0, R₄ is —H, R₈ is—H, and R₉ is -tert-butyl.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is -tert-butyl, and R₉ is —H.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —H, and R₉ is -tert-butyl.

In another embodiment, p and m are 0, R₁ is —CH₃, x is 0, R₄ is —H, R₈is —CH₃, and R₉ is —CH₃.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —H, and R₉ is -halo. Inanother embodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. Inanother embodiment, R₉ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —H, and R₉ is -halo. Inanother embodiment, R₉ is —Cl. In another embodiment, R₉ is —Br. Inanother embodiment, R₉ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is -halo, and R₉ is —H. Inanother embodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. Inanother embodiment, R₈ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is -halo, and R₉ is —H. Inanother embodiment, R₈ is —Cl. In another embodiment, R₈ is —Br. Inanother embodiment, R₈ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —H, and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —H, and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —H, and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —H, and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —CF₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —CF₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —H, and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —H, and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —OCH₂CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —OCH₂CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —H, and R₉ is -halo. Inanother embodiment R₉ is —Cl. In another embodiment, R₉ is —Br. Inanother embodiment, R₉ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is -halo, and R₉ is —H. Inanother embodiment R₈ is —Cl. In another embodiment, R₈ is —Br. Inanother embodiment, R₈ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —H, and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —H, and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —CF₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —H, and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —OCH₂CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —H, and R₉ is -halo. Inanother embodiment R₉ is —Cl. In another embodiment, R₉ is —Br. Inanother embodiment, R₉ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is -halo, and R₉ is —H. Inanother embodiment R₈ is —Cl. In another embodiment, R₈ is —Br. Inanother embodiment, R₈ is —F. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —H, and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichhe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —H, and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —CF₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —H, and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CF₃, x is 0, R₄ is —H, R₃is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the benzooxazolyl group, R₈ is —OCH₂CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₃ is —CH₃and is attached to the carbon atom adjacent to the nitrogen attached tothe benzooxazolyl group, R₄ is —H, R₈ is -tert-butyl, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₃ is —CH₃ andis attached to the carbon atom adjacent to the nitrogen attached to thebenzooxazolyl group, R₄ is —H, R₈ is -tert-butyl, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is -halo, x is 0, R₃ is —CH₃and is attached to the carbon atom adjacent to the nitrogen attached tothe benzooxazolyl group, R₄ is —H, R₈ is —H, and R₉ is -tert-butyl. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration

In another embodiment, p is 0, m is 1, R₁ is —Cl, x is 0, R₃ is —CH₃ andis attached to the carbon atom adjacent to the nitrogen attached to thebenzooxazolyl group, R₄ is —H, R₈ is —H, and R₉ is -tert-butyl. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₃ is —CH₃and is attached to the carbon atom adjacent to the nitrogen attached tothe benzooxazolyl group, R₄ is —H, R₈ is -tert-butyl, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₃ is —CH₃and is attached to the carbon atom adjacent to the nitrogen attached tothe benzooxazolyl group, R₄ is —H, R₈ is —H, and R₉ is -tert-butyl. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, p is 0, m is 1, R₁ is —CH₃, x is 0, R₃ is —CH₃and is attached to the carbon atom adjacent to the nitrogen attached tothe benzooxazolyl group, R₄ is —H, R₈ is —CH₃, and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrazinyl group, p is 0, m is 1, R₁ is—CH₃ or -halo, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached tothe carbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)—group, R₄ is —H, R₈ is —H, and R₉ is -halo. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.In another embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyrazinyl group, p is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —Cl. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyrazinyl group, p is 0, m is 1, R₁ is-halo, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —Br. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyrazinyl group, p is 0, m is 1, R₁ is—Cl, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbonatom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₄ is—H, R₈ is —H, and R₉ is —Br. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyrazinyl group, p is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —F. In another embodiment, the carbon atomto which the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—CH₃or -halo, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached tothe carbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)—group, R₄ is —H, R₈ is —H, and R₉ is -halo. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.In another embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —Cl. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is-halo, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —Br. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—Cl, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbonatom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₄ is—H, R₈ is —H, and R₉ is —Br. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —F. In another embodiment, the carbon atomto which the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—CH₃ or -halo, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached tothe carbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)—group, R₄ is —H, R₈ is —H, and R₉ is -halo. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.In another embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —Cl. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is-halo, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —Br. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—Cl, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to the carbonatom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group, R₄ is—H, R₈ is —H, and R₉ is —Br. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—CH₃, x is 1, A is —C(O)—N(R₄)—, R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— group,R₄ is —H, R₈ is —H, and R₉ is —F. In another embodiment, the carbon atomto which the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyrazinyl group, p is 0, m is 1, R₁ is—CH₃ or -halo, x is 0, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the benzooxazolyl group, R₄ is —H,R₈ is —H, and R₉ is -halo. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyrazinyl group, p is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzooxazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Cl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrazinyl group, p is 0, m is 1, R₁ is-halo, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzooxazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Br. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrazinyl group, p is 0, m is 1, R₁ is—Cl, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzooxazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Br. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrazinyl group, p is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzooxazolyl group, R₄ is —H, R₈ is —H,and R₉ is —F. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—CH₃ or -halo, x is 0, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the benzooxazolyl group, R₄ is —H,R₈ is —H, and R₉ is -halo. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzooxazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Cl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is-halo, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzooxazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Br. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—Cl, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzooxazolyl group, R₄ is —H, R8 is —H,and R₉ is —Br. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridazinyl group, p is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzooxazolyl group, R₄ is —H, R₈ is —H,and R₉ is —F. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—CH₃ or -halo, x is 0, R₃ is —CH₃ and is attached to the carbon atomadjacent to the nitrogen attached to the benzooxazolyl group, R₄ is —H,R₈ is —H, and R₉ is -halo. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzooxazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Cl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is-halo, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzooxazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Br. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—Cl, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzooxazolyl group, R₄ is —H, R₈ is —H,and R₉ is —Br. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a thiazanyl group, p is 0, m is 1, R₁ is—CH₃, x is 0, R₃ is —CH₃ and is attached to the carbon atom adjacent tothe nitrogen attached to the benzooxazolyl group, R₄ is —H, R₈ is —H,and R₉ is —F. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, m is 1 and R₃ is —(C₁—C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)—when x is 1 or the benzooxazolyl group when x is 0. In anotherembodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached to the carbonatom adjacent to the nitrogen attached to the —C(O)—N(R₄)— when x is 1or the benzooxazolyl group when x is 0 and the carbon to which the R₃group is attached is in the R configuration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— when xis 1 or the benzooxazolyl group when x is 0. In another embodiment, m is1 and R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the —C(O)—N(R₄)— when x is 1 or the benzooxazolylgroup when x is 0 and the carbon to which the R₃ group is attached is inthe R configuration.

In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)—when x is 1 or the benzooxazolyl group when x is 0. In anotherembodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached to the carbonatom adjacent to the nitrogen attached to the —C(O)—N(R₄)— when x is 1or the benzooxazolyl group when x is 0 and the carbon to which the R₃group is attached is in the S configuration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the —C(O)—N(R₄)— when xis 1 or the benzooxazolyl group when x is 0. In another embodiment, m is1 and R₃ is —CH₃ and is attached to the carbon atom adjacent to thenitrogen attached to the —C(O)—N(R₄)— when x is 1 or the benzooxazolylgroup when x is 0 and the carbon to which the R₃ group is attached is inthe S configuration.

In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the pyrazinylgroup, pyridazinyl group, or thiazanyl group. In another embodiment, mis 1 and R₃ is —(C₁-C₄)alkyl and is attached to the carbon atom adjacentto the nitrogen attached to the pyrazinyl group, pyridazinyl group, orthiazanyl group and the carbon to which the R₃ group is attached is inthe R configuration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the pyrazinyl group,pyridazinyl group, or thiazanyl group. In another embodiment, m is 1 andR₃ is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the pyrazinyl group, pyridazinyl group, or thiazanyl groupand the carbon to which the R₃ group is attached is in the Rconfiguration.

In another embodiment, m is 1 and R₃ is —(C₁-C₄)alkyl and is attached tothe carbon atom adjacent to the nitrogen attached to the pyrazinylgroup, pyridazinyl group, or thiazanyl group. In another embodiment, mis 1 and R₃ is —(C₁-C₄)alkyl and is attached to the carbon atom adjacentto the nitrogen attached to the pyrazinyl group, pyridazinyl group, orthiazanyl group and the carbon to which the R₃ group is attached is inthe S configuration.

In another embodiment, m is 1 and R₃ is —CH₃ and is attached to thecarbon atom adjacent to the nitrogen attached to the pyrazinyl group,pyridazinyl group, or thiazanyl group. In another embodiment, m is 1 andR₃ is —CH₃ and is attached to the carbon atom adjacent to the nitrogenattached to the pyrazinyl group, pyridazinyl group, or thiazanyl groupand the carbon to which the R₃ group is attached is in the Sconfiguration.

4.7 The Compounds of Formula (IVa)

The present invention also encompasses compounds of formula (IVa):

and pharmaceutically acceptable salts thereof, where Ar₁, Ar₂, and R₃,are defined above for the Benzoazolylpiperazine Compounds of formula(IVa).

In one embodiment, Ar₁ is a pyridyl group.

In another embodiment, Ar₁ is a pyrimidinyl group.

In another embodiment, Ar₂ is a benzothiazolyl group.

In another embodiment, Ar₂ is a benzooxazolyl group.

In another embodiment, Ar₂ is a benzoimidazolyl group.

In another embodiment, n or p is 0.

In another embodiment, n or p is 1.

In another embodiment, R₁ is —Cl.

In another embodiment, R₁ is —Br.

In another embodiment, R₁ is —I.

In another embodiment, R₁ is —F.

In another embodiment, R₁ is —(C₁-C₆)allyl.

In another embodiment, R₁ is —CH₃.

In another embodiment, R₁ is —NO₂.

In another embodiment, R₁ is —CN.

In another embodiment, R₁ is —OH.

In another embodiment, R₁ is —OCH₃.

In another embodiment, R₁ is —NH₂.

In another embodiment, R₁ is —C(halo)₃.

In another embodiment, R₁ is —CH(halo)₂.

In another embodiment, R₁ is —CH₂(halo).

In another embodiment, n and p are 1 and R₂ is -halo, —CN, —OH,—O(C₁-C₆)alkyl, —NO₂, or —NH₂.

In another embodiment, n and p are 1 and R₂ is —(C₁-C₁₀)alkyl,—(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl,—(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,—(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, eachof which is unsubstituted or substituted with one or more R₅ groups.

In another embodiment, n and p are 1 and R₂ is -phenyl, -naphthyl,—(C₁₄)aryl, or -(5- to 10-membered)heteroaryl, each of which isunsubstituted or substituted with one or more R₆ groups;

In another embodiment, R₃ is —H.

In another embodiment, R₃ is —CH₃.

In another embodiment, R₈ and R₉ are each independently —H, halo,—(C₁-C₆)alkyl, —O(C₁-C₆)alkyl, —C(halo)₃, —CH(halo)₂, or —CH₂(halo).

In another embodiment, at least one of R₈ and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or, —I; Ar₂ is a benzothiazolyl group; and R₈ and R₉ are—H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzothiazolyl group; and R₈ and R₉ are —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is-halo.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -chloro.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -bromo.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -fluoro.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -iodo.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -halo; and R₉is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -chloro; andR₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -bromo; and R₉is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -fluoro; andR₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -iodo; and R₉is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzothiazolyl group; R₈ is -halo, and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzothiazolyl group; R₈ is -chloro, and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzothiazolyl group; R₈ is -bromo, and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzothiazolyl group; R₈ is -fluoro, and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzothiazolyl group; R₈ is -iodo, and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is—CH₃.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzothiazolyl group; R₈ is —H, and R₉ is —CH₃.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —CH₃; and R₉is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzothiazolyl group; R₈ is —CH₃, and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is—CF₃.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —CF₃.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —CF₃; and R₉is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzothiazolyl group; R₈ is —CF₃; and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is—OCH₂CH₃.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃.

In another embodiment Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —OCH₂CH₃; andR₉ is —H.

In another embodiment, Ar₁ Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁is —F; Ar₂ is a benzothiazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -tert-butyl;and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzothiazolyl group; R₈ is -tert-butyl; and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ isR₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; andR₉ is -tert-butyl.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ isR₁ is —F; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is-tert-butyl.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or, —I; Ar₂ is a benzothiazolyl group; and R₈ and R₉ are—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzothiazolyl group; and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is-halo. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -chloro. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -bromo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -fluoro. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -halo; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -chloro; andR₉ is —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -bromo; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -fluoro; andR₉ is —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -iodo; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzothiazolyl group; R₈ is -halo, and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzothiazolyl group; R₈ is -chloro, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzothiazolyl group; R₈ is -bromo, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzothiazolyl group; R₈ is -fluoro, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzothiazolyl group; R₈ is -iodo, and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is—CH₃. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzothiazolyl group; R₈ is —H, and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —CH₃; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzothiazolyl group; R₈ is —CH₃, and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is—CF₃. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —CF₃; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzothiazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is—OCH₂CH₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —OCH₂CH₃; andR₉ is —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzothiazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -tert-butyl;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; R₈ is -tert-butyl; and R₉ is —H. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ isR₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; andR₉ is -tert-butyl. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ isR₁ is —F; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is-tert-butyl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or, —I; Ar₂ is a benzothiazolyl group; and R₈ and R₉are —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzothiazolyl group; and R₈ and R₉ are —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉is -halo.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -chloro.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -bromo.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -fluoro.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -iodo.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -halo; andR₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -chloro;and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -bromo; andR₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -fluoro;and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -iodo; andR₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzothiazolyl group; R₈ is -halo, and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzothiazolyl group; R₈ is -chloro, and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzothiazolyl group; R₈ is -bromo, and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzothiazolyl group; R₈ is -fluoro, and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzothiazolyl group; R₈ is -iodo, and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉is —CH₃.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzothiazolyl group; R₈ is —H, and R₉ is —CH₃.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —CH₃; andR₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzothiazolyl group; R₈ is —CH₃, and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉is —CF₃.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —CF₃.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —CF₃; andR₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzothiazolyl group; R₈ is —CF₃; and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉is —OCH₂CH₃.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃.

In another embodiment Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₉ is —OCH₂CH₃;and R₉ is —H.

In another embodiment, Ar₁ Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H;R₁ is —F; Ar₂ is a benzothiazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is-tert-butyl; and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzothiazolyl group; R₈ is -tert-butyl; and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H;and R₉ is -tert-butyl.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is R₁ is —F; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is-tert-butyl.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or, —I; Ar₂ is a benzothiazolyl group; and R₈ and R₉are —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzothiazolyl group; and R₈ and R₉ are —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; andR₉ is -halo. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -chloro. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -bromo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -fluoro. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -iodo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -halo;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -chloro;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -bromo;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -fluoro;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -iodo;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzothiazolyl group; R₈ is -halo, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzothiazolyl group; R₈ is -chloro, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzothiazolyl group; R₈ is -bromo, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzothiazolyl group; R₈ is -fluoro, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzothiazolyl group; R₈ is -iodo, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; andR₉ is —CH₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzothiazolyl group; R₈ is —H, and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —CH₃;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzothiazolyl group; R₈ is —CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; andR₉ is —CF₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —CF₃;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzothiazolyl group; R₈ is —CF₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; andR₉ is —OCH₂CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzothiazolyl group; R₉ is —H; and R₉ is —OCH₂CH₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —OCH₂CH₃;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzothiazolyl group; R₁ is —OCH₂CH₃; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is-tert-butyl; and R₉ is —H. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; R₈ is -tert-butyl; and R₉ is —H. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.In another embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is—H; and R₉ is -tert-butyl. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is R₁ is —F; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is-tert-butyl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or, —I; Ar₂ is a benzoimidazolyl group; and R₈ and R₉ are—H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzoimidazolyl group; and R₈ and R₉ are —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is-halo.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -chloro.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -bromo.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -fluoro.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -iodo.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -halo; and R₉is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -chloro; andR₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -bromo; andR₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -fluoro; andR₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -iodo; and R₉is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzoimidazolyl group; R₈ is -halo, and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzoimidazolyl group; R₈ is -chloro, and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzoimidazolyl group; R₈ is -bromo, and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzoimidazolyl group; R₈ is -fluoro, and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzoimidazolyl group; R₈ is -iodo, and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is—CH₃.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzoimidazolyl group; R₈ is —H, and R₉ is —CH₃.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —CH₃; and R₉is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzoimidazolyl group; R₈ is —CH₃, and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is—CF₃.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —CF₃.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —CF₃; and R₉is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzoimidazolyl group; R₈ is —CF₃; and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is—OCH₂CH₃.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃.

In another embodiment Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —OCH₂CH₃; andR₉ is —H.

In another embodiment, Ar₁ Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁is —F; Ar₂ is a benzoimidazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -tert-butyl;and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzoimidazolyl group; R₈ is -tert-butyl; and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ isR₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; andR₉ is -tert-butyl.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ isR₁ is —F; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is-tert-butyl.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or, —I; Ar₂ is a benzoimidazolyl group; and R₈ and R₉ are—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzoimidazolyl group; and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is-halo. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -chloro. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -bromo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -fluoro. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -iodo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -halo; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -chloro; andR₉ is —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -bromo; andR₉ is —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -fluoro; andR₉ is —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -iodo; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzoimidazolyl group; R₈ is -halo, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzoimidazolyl group; R₈ is -chloro, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzoimidazolyl group; R₈ is -bromo, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzoimidazolyl group; R₈ is -fluoro, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzoimidazolyl group; R₈ is -iodo, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is—CH₃. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzoimidazolyl group; R₈ is —H, and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —CH₃; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzoimidazolyl group; R₈ is —CH₃, and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is—CF₃. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —CF₃; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzoimidazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is—OCH₂CH₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —OCH₂CH₃; andR₉ is —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzoimidazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -tert-butyl;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; R₈ is -tert-butyl; and R₉ is —H. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ isR₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; andR₉ is -tert-butyl. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is-CH₃; R₁ isR₁ is —F; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is-tert-butyl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or, —I; Ar₂ is a benzoimidazolyl group; and R₈ and R₉are —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzoimidazolyl group; and R₈ and R₉ are —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉is -halo.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -chloro.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -bromo.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -fluoro.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -iodo.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -halo; andR₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -chloro;and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -bromo;and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -fluoro;and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -iodo; andR₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzoimidazolyl group; R₈ is -halo, and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzoimidazolyl group; R₈ is -chloro, and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzoimidazolyl group; R₈ is -bromo, and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzoimidazolyl group; R₈ is -fluoro, and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzoimidazolyl group; R₈ is -iodo, and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉is —CH₃.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzoimidazolyl group; R₈ is —H, and R₉ is —CH₃.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —CH₃; andR₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzoimidazolyl group; R₈ is —CH₃, and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉is —CF₃.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —CF₃.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —CF₃; andR₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzoimidazolyl group; R₈ is —CF₃; and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉is —OCH₂CH₃.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃.

In another embodiment Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —OCH₂CH₃;and R₉ is —H.

In another embodiment, Ar₁ Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H;R₁ is —F; Ar₂ is a benzoimidazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is-tert-butyl; and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzoimidazolyl group; R₈ is -tert-butyl; and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H;and R₉ is -tert-butyl.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is R₁ is —F; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is-tert-butyl.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or, —I; Ar₂ is a benzoimidazolyl group; and R₈ andR₉ are —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzoimidazolyl group; and R₈ and R₉ are —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; andR₉ is -halo. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -chloro.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -bromo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -fluoro.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, Ar₂ is a benzoimidazolyl group; Rs is —H; and R₉ is -iodo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -halo;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is-chloro; and R₉ is —H. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -bromo;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is-fluoro; and R₉ is —H. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -iodo;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzoimidazolyl group; R₈ is -halo, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzoimidazolyl group; R₈ is -chloro, and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzoimidazolyl group; R₈ is -bromo, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzoimidazolyl group; R₈ is -fluoro, and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzoimidazolyl group; R₈ is -iodo, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; andR₉ is —CH₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzoimidazolyl group; R₈ is —H, and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —CH₃;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzoimidazolyl group; R₈ is —CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; andR₉ is —CF₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —CF₃;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzoimidazolyl group; R₈ is —CF₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; andR₉ is —OCH₂CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —OCH₂CH₃;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzoimidazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is-tert-butyl; and R₉ is —H. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; R₈ is -tert-butyl; and R₉ is —H. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.In another embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is—H; and R₉ is -tert-butyl. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyriidinyl group, p is 0; R₃ is-CH₃; R₁is R₁ is —F; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is-tert-butyl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or, —I; Ar₂ is a benzooxazolyl group; and R₈ and R₉ are—H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzooxazolyl group; and R₈ and R₉ are —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is-halo.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -chloro.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -bromo.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -fluoro.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -iodo.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -halo; and R₉is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -chloro; and R₉is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -bromo; and R₉is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -fluoro; and R₉is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -iodo; and R₉is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzooxazolyl group; R₈ is -halo, and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzooxazolyl group; R₈ is -chloro, and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzooxazolyl group; R₈ is -bromo, and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzooxazolyl group; R₈ is -fluoro, and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzooxazolyl group; R₈ is -iodo, and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is—CH₃.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzooxazolyl group; R₈ is —H, and R₉ is —CH₃.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —CH₃; and R₉ is—H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzooxazolyl group; R₈ is —CH₃, and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is—CF₃.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CF₃.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —CF₃; and R₉ is—H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzooxazolyl group; R₈ is —CF₃; and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is—OCH₂CH₃.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃.

In another embodiment Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —OCH₂CH₃; andR₉ is —H.

In another embodiment, Ar₁ Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁is —F; Ar₂ is a benzooxazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -tert-butyl;and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ is—F; Ar₂ is a benzooxazolyl group; R₈ is -tert-butyl; and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ isR₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; andR₉ is -tert-butyl.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —H; R₁ isR₁ is —F; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -tert-butyl.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or, —I; Ar₂ is a benzooxazolyl group; and R₈ and R₉ are—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzooxazolyl group; and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is-halo. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -chloro. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -fluoro. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon tom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or I; Ar₂ is a benzooxazolyl group; R₈ is -halo; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -chloro; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -bromo; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -fluoro; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -iodo; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzooxazolyl group; R₈ is -halo, and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzooxazolyl group; R₈ is -chloro, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzooxazolyl group; R₈ is -bromo, and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzooxazolyl group; R₈ is -fluoro, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzooxazolyl group; R₈ is -iodo, and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is—CH₃. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzooxazolyl group; R₈ is —H, and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —CH₃; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzooxazolyl group; R₈ is —CH₃, and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is—CF₃. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —CF₃; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzooxazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is—OCH₂CH₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —OCH₂CH₃; andR₉ is —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; Ar₂ is a benzooxazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -tert-butyl;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ is—F; R₈ is -tert-butyl; and R₉ is —H. In another embodiment, the carbonatom to which the R₃ group is attached has the R configuration. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ isR₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; andR₉ is -tert-butyl. In another embodiment, the carbon atom to which theR₃ group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₃ is —CH₃; R₁ isR₁ is —F; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -tert-butyl.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or, —I; Ar₂ is a benzooxazolyl group; and R₈ and R₉ are—H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzooxazolyl group; and R₈ and R₉ are —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉is -halo.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -chloro.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -bromo.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -fluoro.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -iodo.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -halo; andR₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -chloro; andR₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -bromo; andR₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -fluoro; andR₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -iodo; andR₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzooxazolyl group; R₈ is -halo, and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzooxazolyl group; R₈ is -chloro, and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzooxazolyl group; R₈ is -bromo, and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzooxazolyl group; R₈ is -fluoro, and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzooxazolyl group; R₈ is -iodo, and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉is —CH₃.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzooxazolyl group; R₈ is —H, and R₉ is —CH₃.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —CH₃; and R₉is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzooxazolyl group; R₈ is —CH₃, and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉is —CF₃.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CF₃.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —CF₃; and R₉is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzooxazolyl group; R₈ is —CF₃; and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉is —OCH₂CH₃.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃.

In another embodiment Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —OCH₂CH₃;and R₉ is —H.

In another embodiment, Ar₁ Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H;R₁ is —F; Ar₂ is a benzooxazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -tert-butyl;and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is —F; Ar₂ is a benzooxazolyl group; R₈ is -tert-butyl; and R₉ is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H;and R₉ is -tert-butyl.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —H; R₁is R₁ is —F.; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is-tert-butyl.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or, —I; Ar₂ is a benzooxazolyl group; and R₈ and R₉are —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzooxazolyl group; and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; andR₉ is -halo. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; andR₉ is -chloro. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; andR₉ is -bromo. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; andR₉ is -fluoro. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; andR₉ is -iodo. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -chloro. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -bromo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -fluoro. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -iodo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -halo;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -chloro;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -bromo;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -fluoro;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -iodo;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzooxazolyl group; R₈ is -halo, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzooxazolyl group; R₈ is -chloro, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; 25 Ar₂ is a benzooxazolyl group; R₈ is -bromo, and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzooxazolyl group; R₈ is -fluoro, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzooxazolyl group; R₈ is -iodo, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; andR₉ is —CH₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzooxazolyl group; R₈ is —H, and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —CH₃; andR₉ is —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzooxazolyl group; R₈ is —CH₃, and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; andR₉ is —CF₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —CF₃; andR₉ is —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzooxazolyl group; R₈ is —CF₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; andR₉ is —OCH₂CH₃. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃; R₁is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —OCH₂CH₃;and R₉ is —H. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; Ar₂ is a benzooxazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is-tert-butyl; and R₉ is —H. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is —F; R₈ is -tert-butyl; and R₉ is —H. In another embodiment, thecarbon atom to which the R₃ group is attached has the R configuration.In another embodiment, the carbon atom to which the R₃ group is attachedhas the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is R₁ is —F, —Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H;and R₉ is -tert-butyl. In another embodiment, the carbon atom to whichthe R₃ group is attached has the R configuration. In another embodiment,the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₃ is —CH₃;R₁ is R₁ is —F; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is-tert-butyl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

4.8 The Compounds of Formula (IVb)

The present invention also encompasses compounds of formula (IVb):

and pharmaceutically acceptable salts thereof, where Ar₁, Ar₂, A, R₃ andx are defined above for the Benzoazolylpiperazine Compounds of formula(IVb).

In one embodiment, Ar₁ is a pyridyl group.

In another embodiment, Ar₁ is a pyrimidinyl group.

In another embodiment, n or p is 0.

In another embodiment, n or p is 1.

In another embodiment, x is 0.

In another embodiment, x is 1.

In another embodiment, R₁ is —F.

In another embodiment, R₁ is —Cl.

In another embodiment, R₁ is —Br.

In another embodiment, R₁ is —I.

In another embodiment, R₁ is —(C₁-C₆)alkyl.

In another embodiment, R₁ is —CH₃.

In another embodiment, R₁ is —NO₂.

In another embodiment, R₁ is —CN.

In another embodiment, R₁ is —OH.

In another embodiment, R₁ is —OCH₃.

In another embodiment, R₁ is —NH2.

In another embodiment, R₁ is —C(halo)₃.

In another embodiment, R₁ is —CH(halo)₂.

In another embodiment, R₁ is —CH₂(halo).

In another embodiment, n and p are 1 and R₂ is -halo, —CN, —OH,—O(C₁-C₆)alkyl, —NO₂, or —NH₂.

In another embodiment, n and p are 1 and R₂ is —(C₁-C₁₀)alkyl,—(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl,—(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,—(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, eachof which is unsubstituted or substituted with one or more R₅ groups.

In another embodiment, n and p are 1 and R₂ is -phenyl, -naphthyl,—(C₁₄)aryl, or -(5- to 10-membered)heteroaryl, each of which isunsubstituted or substituted with one or more R₆ groups;

In another embodiment, x is 1 and A is —C(O)N(R₄)—.

In another embodiment, x is 1, A is —C(O)N(R₄)—, and R₄ is —H.

In another embodiment, x is 1, A is —C(O)N(R₄)—, and R₄ is —CH₃.

In another embodiment, x is 1 and A is —C(S)N(R₄)—.

In another embodiment, x is 1, A is —C(S)N(R₄)—, and R₄ is —H.

In another embodiment, x is 1, A is —C(S)N(R₄)—, and R₄ is —CH₃.

In another embodiment, Ar₂ is a benzothiazolyl group.

In another embodiment, Ar₂ is a benzoimidazolyl group.

In another embodiment, Ar₂ is a benzooxazolyl group.

In another embodiment, R₈ and R₉ are each independently —H, halo,—(C₁-C₆)alkyl, —O(C₁-C₆)alkyl, —C(halo)₃, —CH(halo)₂, or —CH₂(halo).

In another embodiment, at least one of R₈ or R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; R₄ is —H; Ar₂ is a benzothiazolyl group; and R₈ and R₉ are—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; R₄ is—H; Ar₂ is a benzothiazolyl group and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -halo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -chloro.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -bromo.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -fluoro.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -iodo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzothiazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzothiazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzothiazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzothiazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzothiazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —C1,—Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -halo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -chloro; and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -bromo; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -fluoro; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -iodo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzothiazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzothiazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzothiazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzothiazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzothiazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzothiazolyl group; R₈ is —H; and R₉ is —CH₃. In another embodiment,the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —CH₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzothiazolyl group; R₈ is —CH₃; and R₉ is —H. In another embodiment,the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzothiazolyl group; R₈ is —H; and R₉ is —CF₃. In another embodiment,the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —CF₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzothiazolyl group; R₈ is —CF₃; and R₉ is —H. In another embodiment,the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzothiazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzothiazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzothiazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzothiazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzothiazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzothiazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzothiazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzothiazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzothiazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzothiazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzothiazolyl group; and R₈ and R₉ are —H. In another embodiment,the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzothiazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzothiazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzothiazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzothiazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzothiazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzothiazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzothiazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzothiazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -tert-butyl; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzothiazolyl group; R₈ is -tert-butyl; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is-tert-butyl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzothiazolyl group; R₈ is —H; and R₉ is -tert-butyl. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzothiazolyl group; R₈ is -tert-butyl; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is -tert-butyl. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzothiazolyl group; R₈ is —CH₃; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; R₄ is —H; Ar₂ is a benzothiazolyl group; and R₈ and R₉are —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; R₄is —H; Ar₂ is a benzothiazolyl group and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is-halo. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is-chloro. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is-bromo. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is-fluoro. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is-iodo. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —Cl;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —Cl;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —Cl;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —Cl;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —Cl;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -halo; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -chloro; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -bromo; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -fluoro; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -iodo; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —CH₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —CH₃; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —CF₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —CF₃; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is—OCH₂CH₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —OCH₂CH₃; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -tert-butyl; andR₉ is —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is -tert-butyl; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is-tert-butyl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₉ is —H; and R₉ is -tert-butyl. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is -tert-butyl; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -tert-butyl. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —CH₃; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; R₄ is —H; Ar₂ is a benzoimidazolyl group; and R₈ and R₉ are—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; R₄ is—H; Ar₂ is a benzoimidazolyl group and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -halo.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -chloro.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -bromo.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -fluoro.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -iodo.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —Cl; Ar₂ isa benzoimidazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —Cl; Ar₂ isa benzoimidazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —Cl; Ar₂ isa benzoimidazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —Cl; Ar₂ isa benzoimidazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —Cl; Ar₂ isa benzoimidazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -halo; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -chloro; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -bromo; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -fluoro; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -iodo; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzoimidazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzoimidazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzoimidazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzoimidazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzoimidazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzoimidazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —CH₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzoimidazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzoimidazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —CF₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzoimidazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzoimidazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzoimidazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzoimidazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzoimidazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzoimidazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzoimidazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzoimidazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzoimidazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzoimidazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzoimidazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzoimidazolyl group; and R₈ and R₉ are —H. In another embodiment,the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzoimidazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzoimidazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzoimidazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzoimidazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzoimidazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzoimidazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzoimidazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzoimidazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -tert-butyl; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Art is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzoimidazolyl group; R₈ is -tert-butyl; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is-tert-butyl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzoimidazolyl group; R₈ is —H; and R₉ is -tert-butyl. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzoimidazolyl group; R₈ is -tert-butyl; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is -tert-butyl. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzoimidazolyl group; R₈ is —CH₃; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; R₄ is —H; Ar₂ is a benzoimidazolyl group; and R₈ and R₉are —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; R₄is —H; Ar₂ is a benzoimidazolyl group and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is-halo. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is-chloro. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is-bromo. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is-fluoro. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is-iodo. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —Cl;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —Cl;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —Cl;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —Cl;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —Cl;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -halo; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -chloro; and R₉is —H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -bromo; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -fluoro; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -iodo; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is—CH₃. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —CH₃; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar1 is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is—CF₃. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —CF₃; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is—OCH₂CH₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —OCH₂CH₃; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₁ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar¹ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -tert-butyl; andR₉ is —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is -tert-butyl; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is-tert-butyl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is -tert-butyl. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is -tert-butyl; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -tert-butyl. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —CH₃; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; R₄ is —H; Ar₂ is a benzooxazolyl group; and R₈ and R₉ are—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; R₄ is—H; Ar₂ is a benzooxazolyl group and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -halo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -chloro.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -bromo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -fluoro.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -iodo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar¹ is a pyridyl group, n is 0; R₁ is —Cl; Ar₂ isa benzooxazolyl group; R₈ is —H; and R₉ is -halo. In another embodiment,the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —Cl; Ar₂ isa benzooxazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —Cl; Ar₂ isa benzooxazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —Cl; Ar₂ isa benzooxazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —Cl; Ar₂ isa benzooxazolyl group; R₈ is —H; and R₉ is -iodo. In another embodiment,the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -halo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -chloro; and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -bromo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -fluoro; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -iodo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzooxazolyl group; R₈ is -halo; and R₉ is —H. In another embodiment,the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzooxazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzooxazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzooxazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzooxazolyl group; R₈ is -iodo; and R₉ is —H. In another embodiment,the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzooxazolyl group; R₈ is —H; and R₉ is —CH₃. In another embodiment,the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —CH₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar1 is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzooxazolyl group; R₈ is —CH₃; and R₉ is —H. In another embodiment,the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzooxazolyl group; R₈ is —H; and R₉ is —CF₃. In another embodiment,the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —CF₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzooxazolyl group; R₈ is —CF₃; and R₉ is —H. In another embodiment,the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzooxazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzooxazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzooxazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzooxazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzooxazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzooxazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzooxazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzooxazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzooxazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzooxazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzooxazolyl group; and R₈ and R₉ are —H. In another embodiment,the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is -chloro. In another.embodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzooxazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzooxazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzooxazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzooxazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzooxazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzooxazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzooxazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CF₃; Ar₂is a benzooxazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -tert-butyl; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzooxazolyl group; R₈ is -tert-butyl; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is-tert-butyl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —F; Ar₂ isa benzooxazolyl group; R₈ is —H; and R₉ is -tert-butyl. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzooxazolyl group; R₈ is -tert-butyl; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is -tert-butyl. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group, n is 0; R₁ is —CH₃; Ar₂is a benzooxazolyl group; R₈ is —CH₃; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; R₄ is —H; Ar₂ is a benzooxazolyl group; and R₈ and R₉are —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; R₄is —H; Ar₂ is a benzooxazolyl group and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F, —Cl—Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -halo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F, —Cl—Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -chloro.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F, —Cl—Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -bromo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F, —Cl—Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -fluoro.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is-iodo. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —Cl;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —Cl;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —Cl;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —Cl;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —Cl;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -halo; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -chloro; and R₉ is—H.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -bromo; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -fluoro; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -iodo; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CH₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —CH₃; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar1 is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CF₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —CF₃; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is—OCH₂CH₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —OCH₂CH₃; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₁ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₁ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -tert-butyl; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is -tert-butyl; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is-tert-butyl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is -tert-butyl. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is -tert-butyl; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -tert-butyl. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyrimidinyl, p is 0; R₁ is —CH₃; Ar₂ isa benzooxazolyl group; R₈ is —CH₃; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; R₄ is —H; Ar₂ is a benzothiazolyl group; and R₈ and R₉ are—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; R₄is —H; Ar₂ is a benzothiazolyl group and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -halo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl—Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -chloro.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -bromo.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl—Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -fluoro.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl—Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -iodo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —Cl; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —Cl; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —Cl; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —Cl; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —Cl; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -halo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -chloro; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ _(i)s a pyridyl group and n is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -bromo; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -fluoro; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -iodo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration. benzothiazolyl group;R₈ is -halo; and R₉ is —H. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —CH₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —CF₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₁ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ _(i)s a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzothiazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -tert-butyl; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is -tert-butyl; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is-tert-butyl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzothiazolyl group; R₈ is —H; and R₉ is -tert-butyl. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is -tert-butyl; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -tert-butyl. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzothiazolyl group; R₈ is —CH₃; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; R₄ is —H; Ar₂ is a benzothiazolyl group; and R₈ and R₉are —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;R₄ is —H; Ar₂ is a benzothiazolyl group and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is-halo. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is-chloro. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is-bromo. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is-fluoro. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is-iodo. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —Cl;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —Cl;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —Cl;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —Cl;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —Cl;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -halo; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -chloro; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -bromo; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -fluoro; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -iodo; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzothiazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzothiazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzothiazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzothiazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzothiazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is—CH₃. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzothiazolyl group; R₁ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —CH₃; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar1 is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzothiazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is—CF₃. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —CF₃; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzothiazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is—OCH₂CH₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —OCH₂CH₃; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzothiazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -halo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -chloro. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -bromo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -fluoro. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -iodo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzothiazolyl group; R₈ is -halo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzothiazolyl group; R₈ is -chloro; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzothiazolyl group; R₈ is -bromo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzothiazolyl group; R₈ is -fluoro; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzothiazolyl group; R₈ is -iodo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzothiazolyl group; R₈ is —CH₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzothiazolyl group; R₈ is —CF₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzothiazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ _(i)s a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzothiazolyl group; and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -halo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -chloro. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -bromo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -fluoro. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -iodo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzothiazolyl group; R₈ is -halo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzothiazolyl group; R₈ is -chloro; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzothiazolyl group; R₈ is -bromo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzothiazolyl group; R₈ is -fluoro; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzothiazolyl group; R₈ is -iodo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzothiazolyl group; R₈ is —CH₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzothiazolyl group; R₈ is —CF₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzothiazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is -tert-butyl; andR₉ is —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzothiazolyl group; R₈ is -tert-butyl; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is-tert-butyl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -tert-butyl. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzothiazolyl group; R₈ is -tert-butyl; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzothiazolyl group; R₈ is —H; and R₉ is -tert-butyl. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzothiazolyl group; R₈ is —CH₃; and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; R₄ is —H; Ar₂ is a benzoimidazolyl group; and R₈ and R₉ are—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; R₄is —H; Ar₂ is a benzoimidazolyl group and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -halo.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -chloro.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -bromo.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -fluoro.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -iodo.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —Cl; Ar₂is a benzoimidazolyi group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —Cl; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —Cl; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —Cl; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —Cl; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -halo; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -chloro; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -bromo; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -fluoro; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -iodo; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration. In another embodiment, Ar₁ isa pyridyl group and n is 0; R₁ is —F; Ar₂ is a benzoimidazolyl group; R₈is -chloro; and R₉ is —H. In another embodiment, the carbon atom towhich the R₃ group is attached has the R configuration. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Sconfiguration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, —I; Ar₂ is a benzoimidazolyl group; R₈ is —CH₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar1 is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —CF₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzoimidazolyl group; R₁ is —H; and R₉ is —OCH₂CH₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl.group and n is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzoimidazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -tert-butyl; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is -tert-butyl; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is-tert-butyl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzoimidazolyl group; R₈ is —H; and R₉ is -tert-butyl. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is -tert-butyl; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -tert-butyl. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzoimidazolyl group; R₈ is —CH₃; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; R₄ is —H; Ar₂ is a benzoimidazolyl group; and R₈ and R₉are —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;R₄ is —H; Ar₂ is a benzoimidazolyl group and R₈ and R₉ are —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is-halo. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is-chloro. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is-bromo. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is-fluoro. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is-iodo. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —Cl;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —Cl;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —Cl;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —Cl;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —Cl;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -halo; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -chloro; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -bromo; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -fluoro; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -iodo; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzoimidazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzoimidazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzoimidazolyl group; R₈ is -bromo; and R₁ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzoimidazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzoimidazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is—CH₃. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —CH₃; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar1 is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzoimidazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is—CF₃. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —CF₃; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzoimidazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is—OCH₂CH₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is —OCH₂CH₃; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzoimidazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -halo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -chloro. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -bromo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -fluoro. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -iodo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzoimidazolyl group; R₈ is -halo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzoimidazolyl group; R₈ is -chloro; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzoimidazolyl group; R₈ is -bromo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzoimidazolyl group; R₈ is -fluoro; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzoimidazolyl group; R₈ is -iodo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzoimidazolyl group; R₈ is —CH₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzoimidazolyl group; R₈ is —CF₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzoimidazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzoimidazolyl group; and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -halo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -chloro. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -bromo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzoimidazolyl group; R₁ is —H; and R₉ is -fluoro. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -iodo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzoimidazolyl group; R₈ is -halo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzoimidazolyl group; R₈ is -chloro; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzoimidazolyl group; R₈ is -bromo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzoimidazolyl group; R₈ is -fluoro; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzoimidazolyl group; R₈ is -iodo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzoimidazolyl group; R₈ is —CH₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzoimidazolyl group; R₈ is —CF₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzoimidazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₈ is -tert-butyl; andR₉ is —H. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzoimidazolyl group; R₈ is -tert-butyl; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzoimidazolyl group; R₁ is —H; and R₉ is-tert-butyl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -tert-butyl. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzoimidazolyl group; R₈ is -tert-butyl; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzoimidazolyl group; R₈ is —H; and R₉ is -tert-butyl.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzoimidazolyl group; R₉ is —CH₃; and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; R₄ is —H; Ar₂ is a benzooxazolyl group; and R₈ and R₉ are—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; R₄is —H; Ar₂ is a benzooxazolyl group and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl—Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -halo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl—Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -chloro.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl—Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -bromo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl—Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -fluoro.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl—Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -iodo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —Cl; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —Cl; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —Cl; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —Cl; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —Cl; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -halo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -chloro; and R₉ is —H.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -bromo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -fluoro; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -iodo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —CH₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₁ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CF₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₁ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —CF₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas.the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₁ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₉ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CF₃;Ar₂ is a benzooxazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -tert-butyl; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is -tert-butyl; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F, —Cl,—Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is-tert-butyl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —F; Ar₂is a benzooxazolyl group; R₈ is —H; and R₉ is -tert-butyl. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is -tert-butyl; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -tert-butyl. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyridyl group and n is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —CH₃; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; R₄ is —H; Ar₂ is a benzooxazolyl group; and R₈ and R₉are —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;R₄ is —H; Ar₂ is a benzooxazolyl group and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is-halo. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is-chloro. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is-bromo. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is-fluoro. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is-iodo. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —Cl;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -halo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —Cl;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -chloro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —Cl;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -bromo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —Cl;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -fluoro. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —Cl;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -iodo. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -halo; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -chloro; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -bromo; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -fluoro; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -iodo; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzooxazolyl group; R₈ is -halo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzooxazolyl group; R₈ is -chloro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzooxazolyl group; R₈ is -bromo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzooxazolyl group; R₈ is -fluoro; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzooxazolyl group; R₈ is -iodo; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CH₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —CH₃; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzooxazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CF₃.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —CF₃; and R₉ is —H.In another embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzooxazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is—OCH₂CH₃. In another embodiment, the carbon atom to which the R₃ groupis attached has the R configuration. In another embodiment, the carbonatom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —OCH₂CH₃; and R₉ is—H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzooxazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -halo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzooxazolyl group; R₈ is —H; and R is -chloro. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -bromo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -fluoro. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -iodo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzooxazolyl group; R₈ is -halo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzooxazolyl group; R₈ is -chloro; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzooxazolyl group; R₈ is -bromo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzooxazolyl group; R₈ is -fluoro; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzooxazolyl group; R₁ is -iodo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzooxazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzooxazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzooxazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzooxazolyl group; and R₈ and R₉ are —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -halo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -chloro. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -bromo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -fluoro. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -iodo. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzooxazolyl group; R₈ is -halo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzooxazolyl group; R₈ is -chloro; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzooxazolyl group; R₈ is -bromo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzooxazolyl group; R₈ is -fluoro; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzooxazolyl group; R₈ is -iodo; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzooxazolyl group; R₈ is —CH₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —CF₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzooxazolyl group; R₈ is —CF₃; and R₉ is —H. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is —OCH₂CH₃. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CF₃; Ar₂ is a benzooxazolyl group; R₈ is —OCH₂CH₃; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is -tert-butyl; and R₉is —H. In another embodiment, the carbon atom to which the R₃ group isattached has the R configuration. In another embodiment, the carbon atomto which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzooxazolyl group; R₈ is -tert-butyl; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F,—Cl, —Br, or —I; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is-tert-butyl. In another embodiment, the carbon atom to which the R₃group is attached has the R configuration. In another embodiment, thecarbon atom to which the R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is —F;Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -tert-butyl. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzooxazolyl group; R₈ is -tert-butyl; and R₉ is —H. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group and p is 0; R₁ is—CH₃; Ar₂ is a benzooxazolyl group; R₈ is —H; and R₉ is -tert-butyl. Inanother embodiment, the carbon atom to which the R₃ group is attachedhas the R configuration. In another embodiment, the carbon atom to whichthe R₃ group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —CH₃; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In another embodiment, Ar₁ is a pyriminidyl group, p is 0; R₁ is —CH₃;Ar₂ is a benzooxazolyl group; R₈ is —CH₃; and R₉ is —CH₃. In anotherembodiment, the carbon atom to which the R₃ group is attached has the Rconfiguration. In another embodiment, the carbon atom to which the R₃group is attached has the S configuration.

In the Benzoazolylpiperazine Compounds the R₃ group can be on any carbonof the piperazine ring. In one embodiment, the R₃ group is attached to acarbon atom adjacent to the nitrogen atom attached to the pyridyl group,pyrimidinyl group, pyrazinyl group, pyridazinyl group, or thiazanylgroup. In another embodiment, the R₃ group is attached to a carbon atomadjacent to the nitrogen atom attached to the -(A)- group, when x is 1;or the R₃ group is attached to the carbon atom adjacent to the nitrogenatom attached to the benzothiazolyl group, the benzoimidazolyl group, orthe benzooxazolyl group, when x is 0.

In one embodiment, wherein the Benzoazolylpiperazine Compound has an R₃group, the carbon atom to which the R₃ group is attached has the (R)configuration. In another embodiment, wherein the BenzoazolylpiperazineCompound has an R₃ group, the carbon atom to which the R₃ group isattached has the (S) configuration.

In another embodiment, the Benzoazolylpiperazine Compound has an R₃group; the R₃ group is attached to a carbon atom adjacent to a nitrogenatom attached to the pyridyl group, pyrimidinyl group, pyrazinyl group,pyridazinyl group, or thiazanyl group; and the carbon to which the R₃group is attached is in the (R) configuration. In another embodiment,the Benzoazolylpiperazine Compound has an R₃ group; the R₃ group isattached to a carbon atom adjacent to a nitrogen attached to the pyridylgroup, pyrimidinyl group, pyrazinyl group, pyridazinyl group, orthiazanyl group; the carbon to which the R₃ group is attached is in the(R) configuration; and R₃ is —(C₁-C₄)alkyl unsubstituted or substitutedwith one or more halo groups. In another embodiment, theBenzoazolylpiperazine Compound has an R₃ group; the R₃ group is attachedto a carbon atom adjacent to a nitrogen attached to the pyridyl group,pyrimidinyl group, pyrazinyl group, pyridazinyl group, or thiazanylgroup; the carbon to which the R₃ group is attached is in the (R)configuration; and R₃ is —CH₃. In another embodiment, theBenzoazolylpiperazine Compound has an R₃ group; the R₃ group is attachedto a carbon atom adjacent to a nitrogen attached to the pyridyl group,pyrimidinyl group, pyrazinyl group, pyridazinyl group, or thiazanylgroup; the carbon to which the R₃ group is attached is in the (R)configuration; and R₃ is —CF₃. In another embodiment, theBenzoazolylpiperazine Compound has an R₃ group; the R₃ group is attachedto a carbon atom adjacent to a nitrogen attached to the pyridyl group,pyrimidinyl group, pyrazinyl group, pyridazinyl group, or thiazanylgroup; the carbon to which the R₃ group is attached is in the (R)configuration; and R₃ is —CH₂CH₃.

In another embodiment, the Benzoazolylpiperazine Compound has an R₃group; the R₃ group is attached to a carbon atom adjacent to a nitrogenatom attached to the -(A)- group, when x is 1; or the R₃ group isattached to the carbon atom adjacent to the nitrogen atom attached tothe benzothiazolyl group, the benzoimidazolyl group, or thebenzooxazolyl group when x is 0; and the carbon to which the R₃ group isattached is in the (R) configuration. In another embodiment, theBenzoazolylpiperazine Compound has an R₃ group; the R₃ group is attachedto a carbon atom adjacent to a nitrogen attached to the -(A)- group,when x is 1; or the R₃ group is attached to the carbon atom adjacent tothe nitrogen atom attached to the benzothiazolyl group, thebenzoimidazolyl group, or the benzooxazolyl group, when x is 0; thecarbon to which the R₃ group is attached is in the (R) configuration;and R₃ is —(C₁-C₄)alkyl unsubstituted or substituted with one or morehalo groups. In another embodiment, the Benzoazolylpiperazine Compoundhas an R₃ group; the R₃ group is attached to a carbon atom adjacent to anitrogen attached to the -(A)- group, when x is 1; or the R₃ group isattached to the carbon atom adjacent to the nitrogen atom attached tothe benzothiazolyl group, the benzoimidazolyl group, or thebenzooxazolyl group when x is 0; the carbon to which the R₃ group isattached is in the (R) configuration; and R₃ is —CH₃. In anotherembodiment, the Benzoazolylpiperazine Compound has an R₃ group; the R₃group is attached to a carbon atom adjacent to a nitrogen attached tothe -(A)- group, when x is 1; or the R₃ group is attached to the carbonatom adjacent to the nitrogen atom attached to the benzothiazolyl group,the benzoimidazolyl group, or the benzooxazolyl group, when x is 0; thecarbon to which the R₃ group is attached is in the (R) configuration;and R₃ is —CF₃. In another embodiment, the BenzoazolylpiperazineCompound has an R₃ group; the R₃ group is attached to a carbon atomadjacent to a nitrogen attached to the -(A)- group, when x is 1; or theR₃ group is attached to the carbon atom adjacent to the nitrogen atomattached to the benzothiazolyl group, the benzoimidazolyl group, or thebenzooxazolyl group, when x is 0; the carbon to which the R₃ group isattached is in the (R) configuration; and R₃ is —CH₂CH₃.

In another embodiment, the Benzoazolylpiperazine Compound has an R₃group; the R₃ group is attached to a carbon atom adjacent to a nitrogenatom attached to the pyridyl group, pyrimidinyl group, pyrazinyl group,pyridazinyl group, or thiazanyl group; and the carbon to which the R₃group is attached is in the (S) configuration. In another embodiment,the Benzoazolylpiperazine Compound has an R₃ group; the R₃ group isattached to a carbon atom adjacent to a nitrogen attached to the pyridylgroup, pyrimidinyl group, pyrazinyl group, pyridazinyl group, orthiazanyl group; the carbon to which the R₃ group is attached is in the(S) configuration; and R₃ is —(C₁-C₄)alkyl unsubstituted or substitutedwith one or more halo groups. In another embodiment, theBenzoazolylpiperazine Compound has an R₃ group; the R₃ group is attachedto a carbon atom adjacent to a nitrogen attached to the pyridyl group,pyrimidinyl group, pyrazinyl group, pyridazinyl group, or thiazanylgroup; the carbon to which the R₃ group is attached is in the (S)configuration; and R₃ is —CH₃. In another embodiment, theBenzoazolylpiperazine Compound has an R₃ group; the R₃ group is attachedto a carbon atom adjacent to a nitrogen attached to the pyridyl group,pyrimidinyl group, pyrazinyl group, pyridazinyl group, or thiazanylgroup; the carbon to which the R₃ group is attached is in the (S)configuration; and R₃ is —CF₃. In another embodiment, theBenzoazolylpiperazine Compound has an R₃ group; the R₃ group is attachedto a carbon atom adjacent to a nitrogen attached to the pyridyl group,pyrimidinyl group, pyrazinyl group, pyridazinyl group, or thiazanylgroup; the carbon to which the R₃ group is attached is in the (S)configuration; and R₃ is —CH₂CH₃.

In another embodiment, the Benzoazolylpiperazine Compound has an R₃groups; the R₃ group is attached to a carbon atom adjacent to a nitrogenatom attached to the -(A)- group, when x is 1; or the R₃ group isattached to the carbon atom adjacent to the nitrogen atom attached tothe benzothiazolyl group, the benzoimidazolyl group, or thebenzooxazolyl group, when x is 0; and the carbon to which the R₃ groupis attached is in the (S) configuration. In another embodiment, theBenzoazolylpiperazine Compound has an R₃ group; the R₃ group is attachedto a carbon atom adjacent to a nitrogen attached to the -(A)- group,when x is 1; or the R₃ group is attached to the carbon atom adjacent tothe nitrogen atom attached to the benzothiazolyl group, thebenzoimidazolyl group, or the benzooxazolyl group, when x is 0; thecarbon to which the R₃ group is attached is in the (S) configuration;and R₃ is —(C₁-C₄)alkyl unsubstituted or substituted with one or morehalo groups. In another embodiment, the Benzoazolylpiperazine Compoundhas an R₃ group; the R₃ group is attached to a carbon atom adjacent to anitrogen attached to the -(A)- group, when x is 1; or the R₃ group isattached to the carbon atom adjacent to the nitrogen atom attached tothe benzothiazolyl group, the benzoimidazolyl group, or thebenzooxazolyl group, when x is 0; the carbon to which the R₃ group isattached is in the (S) configuration; and R₃ is —CH₃. In anotherembodiment, the Benzoazolylpiperazine Compound has an R₃ group; the R₃group is attached to a carbon atom adjacent to a nitrogen attached tothe -(A)- group, when x is 1; or the R₃ group is attached to the carbonatom adjacent to the nitrogen atom attached to the benzothiazolyl group,the benzoimidazolyl group, or the benzooxazolyl group, when x is 0; thecarbon to which the R₃ group is attached is in the (S) configuration;and R₃ is —CF₃. In another embodiment, the BenzoazolylpiperazineCompound has an R₃ group; the R₃ group is attached to a carbon atomadjacent to a nitrogen attached to the -(A)- group, when x is 1; or theR₃ group is attached to the carbon atom adjacent to the nitrogen atomattached to the benzothiazolyl group, the benzoimidazolyl group, or thebenzooxazolyl group, when x is 0; the carbon to which the R₃ group isattached is in the (S) configuration; and R₃ is —CH₂CH₃.

In a preferred embodiment, the R₃ group is attached to a carbon atomadjacent to a nitrogen attached to the -(A)- group, when x is 1; or theR₃ group is attached to the carbon atom adjacent to the nitrogen atomattached to the benzothiazolyl group, the benzoimidazolyl group, or thebenzooxazolyl group, when x is 0; and the R₃ group is a —CH₃. In anotherpreferred embodiment, the R₃ group is attached to a carbon atom adjacentto a nitrogen attached to the -(A)- group, when x is 1; or the R₃ groupis attached to the carbon atom adjacent to the nitrogen atom attached tothe benzothiazolyl group, the benzoimidazolyl group, or thebenzooxazolyl group, when x is 0 and the R₃ group is a —CF₃. In anotherpreferred embodiment, the R₃ group is attached to a carbon atom adjacentto a nitrogen attached to the -(A)- group, when x is 1; or the R₃ groupis attached to the carbon atom adjacent to the nitrogen atom attached tothe benzothiazolyl group, the benzoimidazolyl group, or thebenzooxazolyl group, when x is 0; and the R₃ group is a —CH₂CH₃. Inanother preferred embodiment, the R₃ group is attached to a carbon atomadjacent to a nitrogen attached to the -(A)- group, when x is 1; or theR₃ group is attached to the carbon atom adjacent to the nitrogen atomattached to the benzothiazolyl group, the benzoimidazolyl group, or thebenzooxazolyl group, when x is 0; and the carbon to which the R₃ groupis attached is in the (R) configuration. In another preferredembodiment, the R₃ group is attached to a carbon atom adjacent to anitrogen attached to the -(A)- group, when x is 1; or the R₃ group isattached to the carbon atom adjacent to the nitrogen atom attached tothe benzothiazolyl group, the benzoimidazolyl group, or thebenzooxazolyl group, when x is 0; the carbon to which the R₃ group isattached is in the (R) configuration; and the R₃ group is a —CH₃. Inanother preferred embodiment, the R₃ group is attached to a carbon atomadjacent to a nitrogen attached to the -(A)- group, when x is 1; or theR₃ group is attached to the carbon atom adjacent to the nitrogen atomattached to the benzothiazolyl group, the benzoimidazolyl group, or thebenzooxazolyl group, when x is 0; the carbon to which the R₃ group isattached is in the (R) configuration; and the R₃ group is a —CF₃. Inanother preferred embodiment, the R₃ group is attached to a carbon atomadjacent to a nitrogen attached to the -(A)- group, when x is 1; or theR₃ group is attached to the carbon atom adjacent to the nitrogen atomattached to the benzothiazolyl group, the benzoimidazolyl group, or thebenzooxazolyl group, when x is 0; the carbon to which the R₃ group isattached is in the (R) configuration; and the R₃ group is a —CH₂CH₃.

Illustrative Benzoazolylpiperazine Compounds are listed below in TablesI-XXII:

TABLE I

and pharmaceutically acceptable salts thereof, wherein: Compound Ar₁ R₈R₉ AAA -2-(3-chloropyridyl) —Cl —H AAB -2-(3-chloropyridyl) —Br —H AAC-2-(3-chloropyridyl) —F —H AAD -2-(3-chloropyridyl) —CH₃ —H AAE-2-(3-chloropyridyl) —CF₃ —H AAF -2-(3-chloropyridyl) —OCH₃ —H AAG-2-(3-chloropyridyl) —OCH₂CH₃ —H AAH -2-(3-chloropyridyl) —OCF₃ —H AAI-2-(3-chloropyridyl) -tert-butyl —H AAJ -2-(3-chloropyridyl) -iso-propyl—H AAK -2-(3-chloropyridyl) —CH₃ —CH₃ AAL -2-(3-chloropyridyl) —H —H AAM-2-(3-chloropyridyl) —H —Cl AAN -2-(3-chloropyridyl) —H —Br AAO-2-(3-chloropyridyl) —H —F AAP -2-(3-chloropyridyl) —H —CH₃ AAQ-2-(3-chloropyridyl) —H —CF₃ AAR -2-(3-chloropyridyl) —H —OCH₃ AAS-2-(3-chloropyridyl) —H —OCH₂CH₃ AAT -2-(3-chloropyridyl) —H —OCF₃ AAU-2-(3-chloropyridyl) —H -tert-butyl AAV -2-(3-chloropyridyl) —H-iso-propyl AAW -2-(3-methylpyridyl) —Cl —H AAX -2-(3-methylpyridyl) —Br—H AAY -2-(3-methylpyridyl) —F —H AAZ -2-(3-methylpyridyl) —CH₃ —H ABA-2-(3-methylpyridyl) —CF₃ —H ABB -2-(3-methylpyridyl) —OCH₃ —H ABC-2-(3-methylpyridyl) —OCH₂CH₃ —H ABD -2-(3-methylpyridyl) —OCF₃ —H ABE-2-(3-methylpyridyl) -tert-butyl —H ABF -2-(3-methylpyridyl) -iso-propyl—H ABG -2-(3-methylpyridyl) —CH₃ —CH₃ ABH -2-(3-methylpyridyl) —H —H ABI-2-(3-methylpyridyl) —H —Cl ABJ -2-(3-methylpyridyl) —H —Br ABK-2-(3-methylpyridyl) —H —F ABL -2-(3-methylpyridyl) —H —CH₃ ABM-2-(3-methylpyridyl) —H —CF₃ ABN -2-(3-methylpyridyl) —H —OCH₃ ABO-2-(3-methylpyridyl) —H —OCH₂CH₃ ABP -2-(3-methylpyridyl) —H —OCF₃ ABQ-2-(3-methylpyridyl) —H -tert-butyl ABR -2-(3-methylpyridyl) —H-iso-propyl ABS -2-(3-CF₃-pyridyl) —Cl —H ABT -2-(3-CF₃-pyridyl) —Br —HABU -2-(3-CF₃-pyridyl) —F —H ABV -2-(3-CF₃-pyridyl) —CH₃ —H ABW-2-(3-CF₃-pyridyl) —CF₃ —H ABX -2-(3-CF₃-pyridyl) —OCH₃ —H ABY-2-(3-CF₃-pyridyl) —OCH₂CH₃ —H ABZ -2-(3-CF₃-pyridyl) —OCF₃ —H ACA-2-(3-CF₃-pyridyl) -tert-butyl —H ACB -2-(3-CF₃-pyridyl) -iso-propyl —HACC -2-(3-CF₃-pyridyl) —CH₃ —CH₃ ACD -2-(3-CF₃-pyridyl) —H —H ACE-2-(3-CF₃-pyridyl) —H —Cl ACF -2-(3-CF₃-pyridyl) —H —Br ACG-2-(3-CF₃-pyridyl) —H —F ACH -2-(3-CF₃-pyridyl) —H —CH₃ ACI-2-(3-CF₃-pyridyl) —H —CF₃ ACJ -2-(3-CF₃-pyridyl) —H —OCH₃ ACK-2-(3-CF₃-pyridyl) —H —OCH₂CH₃ ACL -2-(3-CF₃-pyridyl) —H —OCF₃ ACM-2-(3-CF₃-pyridyl) —H -tert-butyl ACN -2-(3-CF₃-pyridyl) —H -iso-propylACO -4-(5-chloropyrimidinyl) —Cl —H ACP -4-(5-chloropyrimidinyl) —Br —HACQ -4-(5-chloropyrimidinyl) —F —H ACR -4-(5-chloropyrimidinyl) —CH₃ —HACS -4-(5-chloropyrimidinyl) —CF₃ —H ACT -4-(5-chloropyrimidinyl) —OCH₃—H ACU -4-(5-chloropyrimidinyl) —OCH₂CH₃ —H ACV -4-(5-chloropyrimidinyl)—OCF₃ —H ACW -4-(5-chloropyrimidinyl) -tert-butyl —H ACX-4-(5-chloropyrimidinyl) -iso-propyl —H ACY -4-(5-chloropyrimidinyl)—CH₃ —CH₃ ACZ -4-(5-chloropyrimidinyl) —H —H ADA-4-(5-chloropyrimidinyl) —H —Cl ADB -4-(5-chloropyrimidinyl) —H —Br ADC-4-(5-chloropyrimidinyl) —H —F ADD -4-(5-chloropyrimidinyl) —H —CH₃ ADE-4-(5-chloropyrimidinyl) —H —CF₃ ADF -4-(5-chloropyrimidinyl) —H —OCH₃ADG -4-(5-chloropyrimidinyl) —H —OCH₂CH₃ ADH -4-(5-chloropyrimidinyl) —H—OCF₃ ADI -4-(5-chloropyrimidinyl) —H -tert-butyl ADJ-4-(5-chloropyrimidinyl) —H -iso-propyl ADK -4-(5-methylpyrimidinyl) —Cl—H ADL -4-(5-methylpyrimidinyl) —Br —H ADM -4-(5-methylpyrimidinyl) —F—H ADN -4-(5-methylpyrimidinyl) —CH₃ —H ADO -4-(5-methylpyrimidinyl)—CF₃ —H ADP -4-(5-methylpyrimidinyl) —OCH₃ —H ADQ-4-(5-methylpyrimidinyl) —OCH₂CH₃ —H ADR -4-(5-methylpyrimidinyl) —OCF₃—H ADS -4-(5-methylpyrimidinyl) -tert-butyl —H ADT-4-(5-methylpyrimidinyl) -iso-propyl —H ADU -4-(5-methylpyrimidinyl)—CH₃ —CH₃ ADV -4-(5-methylpyrimidinyl) —H —H ADW-4-(5-methylpyrimidinyl) —H —Cl ADX -4-(5-methylpyrimidinyl) —H —Br ADY-4-(5-methylpyrimidinyl) —H —F ADZ -4-(5-methylpyrimidinyl) —H —CH₃ AEA-4-(5-methylpyrimidinyl) —H —CF₃ AEB -4-(5-methylpyrimidinyl) —H —OCH₃AEC -4-(5-methylpyrimidinyl) —H —OCH₂CH₃ AED -4-(5-methylpyrimidinyl) —H—OCF₃ AEE -4-(5-methylpyrimidinyl) —H -tert-butyl AEF-4-(5-methylpyrimidinyl) —H -iso-propyl AEG -2-pyrazinyl —Cl —H AEH-2-pyrazinyl —Br —H AEI -2-pyrazinyl —F —H AEJ -2-pyrazinyl —CH₃ —H AEK-2-pyrazinyl —CF₃ —H AEL -2-pyrazinyl —OCH₃ —H AEM -2-pyrazinyl —OCH₂CH₃—H AEN -2-pyrazinyl —OCF₃ —H AEO -2-pyrazinyl -tert-butyl —H AEP-2-pyrazinyl -iso-propyl —H AEQ -2-pyrazinyl —CH₃ —CH₃ AER -2-pyrazinyl—H —H AES -2-pyrazinyl —H —Cl AET -2-pyrazinyl —H —Br AEU -2-pyrazinyl—H —F AEV -2-pyrazinyl —H —CH₃ AEW -2-pyrazinyl —H —CF₃ AEX -2-pyrazinyl—H —OCH₃ AEY -2-pyrazinyl —H —OCH₂CH₃ AEZ -2-pyrazinyl —H —OCF₃ AFA-2-pyrazinyl —H -tert-butyl AFB -2-pyrazinyl —H -iso-propyl AFC-2-(3-chloropyrazinyl) —Cl —H AFD -2-(3-chloropyrazinyl) —Br —H AFE-2-(3-chloropyrazinyl) —F —H AFF -2-(3-chloropyrazinyl) —CH₃ —H AFG-2-(3-chloropyrazinyl) —CF₃ —H AFH -2-(3-chloropyrazinyl) —OCH₃ —H AFI-2-(3-chloropyrazinyl) —OCH₂CH₃ —H AFJ -2-(3-chloropyrazinyl) —OCF₃ —HAFK -2-(3-chloropyrazinyl) -tert-butyl —H AFL -2-(3-chloropyrazinyl)-iso-propyl —H AFM -2-(3-chloropyrazinyl) —CH₃ —CH₃ AFN-2-(3-chloropyrazinyl) —H —H AFO -2-(3-chloropyrazinyl) —H —Cl AFP-2-(3-chloropyrazinyl) —H —Br AFQ -2-(3-chloropyrazinyl) —H —F AFR-2-(3-chloropyrazinyl) —H —CH₃ AFS -2-(3-chloropyrazinyl) —H —CF₃ AFT-2-(3-chloropyrazinyl) —H —OCH₃ AFU -2-(3-chloropyrazinyl) —H —OCH₂CH₃AFV -2-(3-chloropyrazinyl) —H —OCF₃ AFW -2-(3-chloropyrazinyl) —H-tert-butyl AFX -2-(3-chloropyrazinyl) —H -iso-propyl AFY-2-(3-methylpyrazinyl) —Cl —H AFZ -2-(3-methylpyrazinyl) —Br —H AGA-2-(3-methylpyrazinyl) —F —H AGB -2-(3-methylpyrazinyl) —CH₃ —H AGC-2-(3-methylpyrazinyl) —CF₃ —H AGD -2-(3-methylpyrazinyl) —OCH₃ —H AGE-2-(3-methylpyrazinyl) —OCH₂CH₃ —H AGF -2-(3-methylpyrazinyl) —OCF₃ —HAGG -2-(3-methylpyrazinyl) -tert-butyl —H AGH -2-(3-methylpyrazinyl)-iso-propyl —H AGI -2-(3-methylpyrazinyl) —CH₃ —CH₃ AGJ-2-(3-methylpyrazinyl) —H —H AGK -2-(3-methylpyrazinyl) —H —Cl AGL-2-(3-methylpyrazinyl) —H —Br AGM -2-(3-methylpyrazinyl) —H —F AGN-2-(3-methylpyrazinyl) —H —CH₃ AGO -2-(3-methylpyrazinyl) —H —CF₃ AGP-2-(3-methylpyrazinyl) —H —OCH₃ AGQ -2-(3-methylpyrazinyl) —H —OCH₂CH₃AGR -2-(3-methylpyrazinyl) —H —OCF₃ AGS -2-(3-methylpyrazinyl) —H-tert-butyl AGT -2-(3-methylpyrazinyl) —H -iso-propyl AGU -2-pyridazinyl—Cl —H AGV -2-pyridazinyl —Br —H AGW -2-pyridazinyl —F —H AGX-2-pyridazinyl —CH₃ —H AGY -2-pyridazinyl —CF₃ —H AGZ -2-pyridazinyl—OCH₃ —H AHA -2-pyridazinyl —OCH₂CH₃ —H AHB -2-pyridazinyl —OCF₃ —H AHC-2-pyridazinyl -tert-butyl —H AHD -2-pyridazinyl -iso-propyl —H AHE-2-pyridazinyl —CH₃ —CH₃ AHF -2-pyridazinyl —H —H AHG -2-pyridazinyl —H—Cl AHH -2-pyridazinyl —H —Br AHI -2-pyridazinyl —H —F AHJ-2-pyridazinyl —H —CH₃ AHK -2-pyridazinyl —H —CF₃ AHL -2-pyridazinyl —H—OCH₃ AHM -2-pyridazinyl —H —OCH₂CH₃ AHN -2-pyridazinyl —H —OCF₃ AHO-2-pyridazinyl —H -tert-butyl AHP -2-pyridazinyl —H -iso-propyl AHQ-3-(4-chloropyridazinyl) —Cl —H AHR -3-(4-chloropyridazinyl) —Br —H AHS-3-(4-chloropyridazinyl) —F —H AHT -3-(4-chloropyridazinyl) —CH₃ —H AHU-3-(4-chloropyridazinyl) —CF₃ —H AHV -3-(4-chloropyridazinyl) —OCH₃ —HAHW -3-(4-chloropyridazinyl) —OCH₂CH₃ —H AHX -3-(4-chloropyridazinyl)—OCF₃ —H AHY -3-(4-chloropyridazinyl) -tert-butyl —H AHZ-3-(4-chloropyridazinyl) -iso-propyl —H AIA -3-(4-chloropyridazinyl)—CH₃ —CH₃ AIB -3-(4-chloropyridazinyl) —H —H AIC-3-(4-chloropyridazinyl) —H —Cl AID -3-(4-chloropyridazinyl) —H —Br AIE-3-(4-chloropyridazinyl) —H —F AIF -3-(4-chloropyridazinyl) —H —CH₃ AIG-3-(4-chloropyridazinyl) —H —CF₃ AIH -3-(4-chloropyridazinyl) —H —OCH₃AII -3-(4-chloropyridazinyl) —H —OCH₂CH₃ AIJ -3-(4-chloropyridazinyl) —H—OCF₃ AIK -3-(4-chloropyridazinyl) —H -tert-butyl AIL-3-(4-chloropyridazinyl) —H -iso-propyl AIM -3-(4-methylpyridazinyl) —Cl—H AIN -3-(4-methylpyridazinyl) —Br —H AIO -3-(4-methylpyridazinyl) —F—H AIP -3-(4-methylpyridazinyl) —CH₃ —H AIQ -3-(4-methylpyridazinyl)—CF₃ —H AIR -3-(4-methylpyridazinyl) —OCH₃ —H AIS-3-(4-methylpyridazinyl) —OCH₂CH₃ —H AIT -3-(4-methylpyridazinyl) —OCF₃—H AIU -3-(4-methylpyridazinyl) -tert-butyl —H AIV-3-(4-methylpyridazinyl) -iso-propyl —H AIW -3-(4-methylpyridazinyl)—CH₃ —CH₃ AIX -3-(4-methylpyridazinyl) —H —H AIY-3-(4-methylpyridazinyl) —H —Cl AIZ -3-(4-methylpyridazinyl) —H —Br AJA-3-(4-methylpyridazinyl) —H —F AJB -3-(4-methylpyridazinyl) —H —CH₃ AJC-3-(4-methylpyridazinyl) —H —CF₃ AJD -3-(4-methylpyridazinyl) —H —OCH₃AJE -3-(4-methylpyridazinyl) —H —OCH₂CH₃ AJF -3-(4-methylpyridazinyl) —H—OCF₃ AJG -3-(4-methylpyridazinyl) —H -tert-butyl AJH-3-(4-methylpyridazinyl) —H -iso-propyl AJI -4-thiazanyl —Cl —H AJJ-4-thiazanyl —Br —H AJK -4-thiazanyl —F —H AJL -4-thiazanyl —CH₃ —H AJM-4-thiazanyl —CF₃ —H AJN -4-thiazanyl —OCH₃ —H AJO -4-thiazanyl —OCH₂CH₃—H AJP -4-thiazanyl —OCF₃ —H AJQ -4-thiazanyl -tert-butyl —H AJR-4-thiazanyl -iso-propyl —H AJS -4-thiazanyl —CH₃ —CH₃ AJT -4-thiazanyl—H —H AJU -4-thiazanyl —H —Cl AJV -4-thiazanyl —H —Br AJW -4-thiazanyl—H —F AJX -4-thiazanyl —H —CH₃ AJY -4-thiazanyl —H —CF₃ AJZ -4-thiazanyl—H —OCH₃ AKA -4-thiazanyl —H —OCH₂CH₃ AKB -4-thiazanyl —H —OCF₃ AKC-4-thiazanyl —H -tert-butyl AKD -4-thiazanyl —H -iso-propyl AKE-5-(4-chlorothiazanyl) —Cl —H AKF -5-(4-chlorothiazanyl) —Br —H AKG-5-(4-chlorothiazanyl) —F —H AKH -5-(4-chlorothiazanyl) —CH₃ —H AKI-5-(4-chlorothiazanyl) —CF₃ —H AKJ -5-(4-chlorothiazanyl) —OCH₃ —H AKK-5-(4-chlorothiazanyl) —OCH₂CH₃ —H AKL -5-(4-chlorothiazanyl) —OCF₃ —HAKM -5-(4-chlorothiazanyl) -tert-butyl —H AKN -5-(4-chlorothiazanyl)-iso-propyl —H AKO -5-(4-chlorothiazanyl) —CH₃ —CH₃ AKP-5-(4-chlorothiazanyl) —H —H AKQ -5-(4-chlorothiazanyl) —H —Cl AKR-5-(4-chlorothiazanyl) —H —Br AKS -5-(4-chlorothiazanyl) —H —F AKT-5-(4-chlorothiazanyl) —H —CH₃ AKU -5-(4-chlorothiazanyl) —H —CF₃ AKV-5-(4-chlorothiazanyl) —H —OCH₃ AKW -5-(4-chlorothiazanyl) —H —OCH₂CH₃AKX -5-(4-chlorothiazanyl) —H —OCF₃ AKY -5-(4-chlorothiazanyl) —H-tert-butyl AKZ -5-(4-chlorothiazanyl) —H -iso-propyl ALA-5-(4-methylthiazanyl) —Cl —H ALB -5-(4-methylthiazanyl) —Br —H ALC-5-(4-methylthiazanyl) —F —H ALD -5-(4-methylthiazanyl) —CH₃ —H ALE-5-(4-methylthiazanyl) —CF₃ —H ALF -5-(4-methylthiazanyl) —OCH₃ —H ALG-5-(4-methylthiazanyl) —OCH₂CH₃ —H ALH -5-(4-methylthiazanyl) —OCF₃ —HALI -5-(4-methylthiazanyl) -tert-butyl —H ALJ -5-(4-methylthiazanyl)-iso-propyl —H ALK -5-(4-methylthiazanyl) —CH₃ —CH₃ ALL-5-(4-methylthiazanyl) —H —H ALM -5-(4-methylthiazanyl) —H —Cl ALN-5-(4-methylthiazanyl) —H —Br ALO -5-(4-methylthiazanyl) —H —F ALP-5-(4-methylthiazanyl) —H —CH₃ ALQ -5-(4-methylthiazanyl) —H —CF₃ ALR-5-(4-methylthiazanyl) —H —OCH₃ ALS -5-(4-methylthiazanyl) —H —OCH₂CH₃ALT -5-(4-methylthiazanyl) —H —OCF₃ ALU -5-(4-methylthiazanyl) —H-tert-butyl ALV -5-(4-methylthiazanyl) —H -iso-propyl

TABLE II

and pharmaceutically acceptable salts thereof, wherein: Compound Ar₁ R₈R₉ ALW -2-(3-chloropyridyl) —Cl —H ALX -2-(3-chloropyridyl) —Br —H ALY-2-(3-chloropyridyl) —F —H ALZ -2-(3-chloropyridyl) —CH₃ —H AMA-2-(3-chloropyridyl) —CF₃ —H AMB -2-(3-chloropyridyl) —OCH₃ —H AMC-2-(3-chloropyridyl) —OCH₂CH₃ —H AMD -2-(3-chloropyridyl) —OCF₃ —H AME-2-(3-chloropyridyl) -tert-butyl —H AMF -2-(3-chloropyridyl) -iso-propyl—H AMG -2-(3-chloropyridyl) —CH₃ —CH₃ AMH -2-(3-chloropyridyl) —H —H AMI-2-(3-chloropyridyl) —H —Cl AMJ -2-(3-chloropyridyl) —H —Br AMK-2-(3-chloropyridyl) —H —F AML -2-(3-chloropyridyl) —H —CH₃ AMM-2-(3-chloropyridyl) —H —CF₃ AMN -2-(3-chloropyridyl) —H —OCH₃ AMO-2-(3-chloropyridyl) —H —OCH₂CH₃ AMP -2-(3-chloropyridyl) —H —OCF₃ AMQ-2-(3-chloropyridyl) —H -tert-butyl AMR -2-(3-chloropyridyl) —H-iso-propyl AMS -2-(3-methylpyridyl) —Cl —H AMT -2-(3-methylpyridyl) —Br—H AMU -2-(3-methylpyridyl) —F —H AMV -2-(3-methylpyridyl) —CH₃ —H AMW-2-(3-methylpyridyl) —CF₃ —H AMX -2-(3-methylpyridyl) —OCH₃ —H AMY-2-(3-methylpyridyl) —OCH₂CH₃ —H AMZ -2-(3-methylpyridyl) —OCF₃ —H ANA-2-(3-methylpyridyl) -tert-butyl —H ANB -2-(3-methylpyridyl) -iso-propyl—H ANC -2-(3-methylpyridyl) —CH₃ —CH₃ AND -2-(3-methylpyridyl) —H —H ANE-2-(3-methylpyridyl) —H —Cl ANF -2-(3-methylpyridyl) —H —Br ANG-2-(3-methylpyridyl) —H —F ANH -2-(3-methylpyridyl) —H —CH₃ ANI-2-(3-methylpyridyl) —H —CF₃ ANJ -2-(3-methylpyridyl) —H —OCH₃ ANK-2-(3-methylpyridyl) —H —OCH₂CH₃ ANL -2-(3-methylpyridyl) —H —OCF₃ ANM-2-(3-methylpyridyl) —H -tert-butyl ANN -2-(3-methylpyridyl) —H-iso-propyl ANO -2-(3-CF₃-pyridyl) —Cl —H ANP -2-(3-CF₃-pyridyl) —Br —HANQ -2-(3-CF₃-pyridyl) —F —H ANR -2-(3-CF₃-pyridyl) —CH₃ —H ANS-2-(3-CF₃-pyridyl) —CF₃ —H ANT -2-(3-CF₃-pyridyl) —OCH₃ —H ANU-2-(3-CF₃-pyridyl) —OCH₂CH₃ —H ANV -2-(3-CF₃-pyridyl) —OCF₃ —H ANW-2-(3-CF₃-pyridyl) -tert-butyl —H ANX -2-(3-CF₃-pyridyl) -iso-propyl —HANY -2-(3-CF₃-pyridyl) —CH₃ —CH₃ ANZ -2-(3-CF₃-pyridyl) —H —H AOA-2-(3-CF₃-pyridyl) —H —Cl AOB -2-(3-CF₃-pyridyl) —H —Br AOC-2-(3-CF₃-pyridyl) —H —F AOD -2-(3-CF₃-pyridyl) —H —CH₃ AOE-2-(3-CF₃-pyridyl) —H —CF₃ AOF -2-(3-CF₃-pyridyl) —H —OCH₃ AOG-2-(3-CF₃-pyridyl) —H —OCH₂CH₃ AOH -2-(3-CF₃-pyridyl) —H —OCF₃ AOI-2-(3-CF₃-pyridyl) —H -tert-butyl AOJ -2-(3-CF₃-pyridyl) —H -iso-propylAOK -4-(5-chloropyrimidinyl) —Cl —H AOL -4-(5-chloropyrimidinyl) —Br —HAOM -4-(5-chloropyrimidinyl) —F —H AON -4-(5-chloropyrimidinyl) —CH₃ —HAOO -4-(5-chloropyrimidinyl) —CF₃ —H AOP -4-(5-chloropyrimidinyl) —OCH₃—H AOQ -4-(5-chloropyrimidinyl) —OCH₂CH₃ —H AOR -4-(5-chloropyrimidinyl)—OCF₃ —H AOS -4-(5-chloropyrimidinyl) -tert-butyl —H AOT-4-(5-chloropyrimidinyl) -iso-propyl —H AOU -4-(5-chloropyrimidinyl)—CH₃ —CH₃ AOV -4-(5-chloropyrimidinyl) —H —H AOW-4-(5-chloropyrimidinyl) —H —Cl AOX -4-(5-chloropyrimidinyl) —H —Br AOY-4-(5-chloropyrimidinyl) —H —F AOZ -4-(5-chloropyrimidinyl) —H —CH₃ APA-4-(5-chloropyrimidinyl) —H —CF₃ APB -4-(5-chloropyrimidinyl) —H —OCH₃APC -4-(5-chloropyrimidinyl) —H —OCH₂CH₃ APD -4-(5-chloropyrimidinyl) —H—OCF₃ APE -4-(5-chloropyrimidinyl) —H -tert-butyl APF-4-(5-chloropyrimidinyl) —H -iso-propyl APG -4-(5-methylpyrimidinyl) —Cl—H APH -4-(5-methylpyrimidinyl) —Br —H API -4-(5-methylpyrimidinyl) —F—H APJ -4-(5-methylpyrimidinyl) —CH₃ —H APK -4-(5-methylpyrimidinyl)—CF₃ —H APL -4-(5-methylpyrimidinyl) —OCH₃ —H APM-4-(5-methylpyrimidinyl) —OCH₂CH₃ —H APN -4-(5-methylpyrimidinyl) —OCF₃—H APO -4-(5-methylpyrimidinyl) -tert-butyl —H APP-4-(5-methylpyrimidinyl) -iso-propyl —H APQ -4-(5-methylpyrimidinyl)—CH₃ —CH₃ APR -4-(5-methylpyrimidinyl) —H —H APS-4-(5-methylpyrimidinyl) —H —Cl APT -4-(5-methylpyrimidinyl) —H —Br APU-4-(5-methylpyrimidinyl) —H —F APV -4-(5-methylpyrimidinyl) —H —CH₃ APW-4-(5-methylpyrimidinyl) —H —CF₃ APX -4-(5-methylpyrimidinyl) —H —OCH₃APY -4-(5-methylpyrimidinyl) —H —OCH₂CH₃ APZ -4-(5-methylpyrimidinyl) —H—OCF₃ AQA -4-(5-methylpyrimidinyl) —H -tert-butyl AQB-4-(5-methylpyrimidinyl) —H -iso-propyl AQC -2-pyrazinyl —Cl —H AQD-2-pyrazinyl —Br —H AQE -2-pyrazinyl —F —H AQF -2-pyrazinyl —CH₃ —H AQG-2-pyrazinyl —CF₃ —H AQH -2-pyrazinyl —OCH₃ —H AQI -2-pyrazinyl —OCH₂CH₃—H AQJ -2-pyrazinyl —OCF₃ —H AQK -2-pyrazinyl -tert-butyl —H AQL-2-pyrazinyl -iso-propyl —H AQM -2-pyrazinyl —CH₃ —CH₃ AQN -2-pyrazinyl—H —H AQO -2-pyrazinyl —H —Cl AQP -2-pyrazinyl —H —Br AQQ -2-pyrazinyl—H —F AQR -2-pyrazinyl —H —CH₃ AQS -2-pyrazinyl —H —CF₃ AQT -2-pyrazinyl—H —OCH₃ AQU -2-pyrazinyl —H —OCH₂CH₃ AQV -2-pyrazinyl —H —OCF₃ AQW-2-pyrazinyl —H -tert-butyl AQX -2-pyrazinyl —H -iso-propyl AQY-2-(3-chloropyrazinyl) —Cl —H AQZ -2-(3-chloropyrazinyl) —Br —H ARA-2-(3-chloropyrazinyl) —F —H ARB -2-(3-chloropyrazinyl) —CH₃ —H ARC-2-(3-chloropyrazinyl) —CF₃ —H ARD -2-(3-chloropyrazinyl) —OCH₃ —H ARE-2-(3-chloropyrazinyl) —OCH₂CH₃ —H ARF -2-(3-chloropyrazinyl) —OCF₃ —HARG -2-(3-chloropyrazinyl) -tert-butyl —H ARH -2-(3-chloropyrazinyl)-iso-propyl —H ARI -2-(3-chloropyrazinyl) —CH₃ —CH₃ ARJ-2-(3-chloropyrazinyl) —H —H ARK -2-(3-chloropyrazinyl) —H —Cl ARL-2-(3-chloropyrazinyl) —H —Br ARM -2-(3-chloropyrazinyl) —H —F ARN-2-(3-chloropyrazinyl) —H —CH₃ ARO -2-(3-chloropyrazinyl) —H —CF₃ ARP-2-(3-chloropyrazinyl) —H —OCH₃ ARQ -2-(3-chloropyrazinyl) —H —OCH₂CH₃ARR -2-(3-chloropyrazinyl) —H —OCF₃ ARS -2-(3-chloropyrazinyl) —H-tert-butyl ART -2-(3-chloropyrazinyl) —H -iso-propyl ARU-2-(3-methylpyrazinyl) —Cl —H ARV -2-(3-methylpyrazinyl) —Br —H ARW-2-(3-methylpyrazinyl) —F —H ARX -2-(3-methylpyrazinyl) —CH₃ —H ARY-2-(3-methylpyrazinyl) —CF₃ —H ARZ -2-(3-methylpyrazinyl) —OCH₃ —H ASA-2-(3-methylpyrazinyl) —OCH₂CH₃ —H ASB -2-(3-methylpyrazinyl) —OCF₃ —HASC -2-(3-methylpyrazinyl) -tert-butyl —H ASD -2-(3-methylpyrazinyl)-iso-propyl —H ASE -2-(3-methylpyrazinyl) —CH₃ —CH₃ ASF-2-(3-methylpyrazinyl) —H —H ASG -2-(3-methylpyrazinyl) —H —Cl ASH-2-(3-methylpyrazinyl) —H —Br ASI -2-(3-methylpyrazinyl) —H —F ASJ-2-(3-methylpyrazinyl) —H —CH₃ ASK -2-(3-methylpyrazinyl) —H —CF₃ ASL-2-(3-methylpyrazinyl) —H —OCH₃ ASM -2-(3-methylpyrazinyl) —H —OCH₂CH₃ASN -2-(3-methylpyrazinyl) —H —OCF₃ ASO -2-(3-methylpyrazinyl) —H-tert-butyl ASP -2-(3-methylpyrazinyl) —H -iso-propyl ASQ -2-pyridazinyl—Cl —H ASR -2-pyridazinyl —Br —H ASS -2-pyridazinyl —F —H AST-2-pyridazinyl —CH₃ —H ASU -2-pyridazinyl —CF₃ —H ASV -2-pyridazinyl—OCH₃ —H ASW -2-pyridazinyl —OCH₂CH₃ —H ASX -2-pyridazinyl —OCF₃ —H ASY-2-pyridazinyl -tert-butyl —H ASZ -2-pyridazinyl -iso-propyl —H ATA-2-pyridazinyl —CH₃ —CH₃ ATB -2-pyridazinyl —H —H ATC -2-pyridazinyl —H—Cl ATD -2-pyridazinyl —H —Br ATE -2-pyridazinyl —H —F ATF-2-pyridazinyl —H —CH₃ ATG -2-pyridazinyl —H —CF₃ ATH -2-pyridazinyl —H—OCH₃ ATI -2-pyridazinyl —H —OCH₂CH₃ ATJ -2-pyridazinyl —H —OCF₃ ATK-2-pyridazinyl —H -tert-butyl ATL -2-pyridazinyl —H -iso-propyl ATM-3-(4-chloropyridazinyl) —Cl —H ATN -3-(4-chloropyridazinyl) —Br —H ATO-3-(4-chloropyridazinyl) —F —H ATP -3-(4-chloropyridazinyl) —CH₃ —H ATQ-3-(4-chloropyridazinyl) —CF₃ —H ATR -3-(4-chloropyridazinyl) —OCH₃ —HATS -3-(4-chloropyridazinyl) —OCH₂CH₃ —H ATT -3-(4-chloropyridazinyl)—OCF₃ —H ATU -3-(4-chloropyridazinyl) -tert-butyl —H ATV-3-(4-chloropyridazinyl) -iso-propyl —H ATW -3-(4-chloropyridazinyl)—CH₃ —CH₃ ATX -3-(4-chloropyridazinyl) —H —H ATY-3-(4-chloropyridazinyl) —H —Cl ATZ -3-(4-chloropyridazinyl) —H —Br AUA-3-(4-chloropyridazinyl) —H —F AUB -3-(4-chloropyridazinyl) —H —CH₃ AUG-3-(4-chloropyridazinyl) —H —CF₃ AUD -3-(4-chloropyridazinyl) —H —OCH₃AUE -3-(4-chloropyridazinyl) —H —OCH₂CH₃ AUF -3-(4-chloropyridazinyl) —H—OCF₃ AUG -3-(4-chloropyridazinyl) —H -tert-butyl AUH-3-(4-chloropyridazinyl) —H -iso-propyl AUI -3-(4-methylpyridazinyl) —Cl—H AUJ -3-(4-methylpyridazinyl) —Br —H AUK -3-(4-methylpyridazinyl) —F—H AUL -3-(4-methylpyridazinyl) —CH₃ —H AUM -3-(4-methylpyridazinyl)—CF₃ —H AUN -3-(4-methylpyridazinyl) —OCH₃ —H AUO-3-(4-methylpyridazinyl) —OCH₂CH₃ —H AUP -3-(4-methylpyridazinyl) —OCF₃—H AUQ -3-(4-methylpyridazinyl) -tert-butyl —H AUR-3-(4-methylpyridazinyl) -iso-propyl —H AUS -3-(4-methylpyridazinyl)—CH₃ —CH₃ AUT -3-(4-methylpyridazinyl) —H —H AUU-3-(4-methylpyridazinyl) —H —Cl AUV -3-(4-methylpyridazinyl) —H —Br AUW-3-(4-methylpyridazinyl) —H —F AUX -3-(4-methylpyridazinyl) —H —CH₃ AUY-3-(4-methylpyridazinyl) —H —CF₃ AUZ -3-(4-methylpyridazinyl) —H —OCH₃AVA -3-(4-methylpyridazinyl) —H —OCH₂CH₃ AVB -3-(4-methylpyridazinyl) —H—OCF₃ AVC -3-(4-methylpyridazinyl) —H -tert-butyl AVD-3-(4-methylpyridazinyl) —H -iso-propyl AVE -4-thiazanyl —Cl —H AVF-4-thiazanyl —Br —H AVG -4-thiazanyl —F —H AVH -4-thiazanyl —CH₃ —H AVI-4-thiazanyl —CF₃ —H AVJ -4-thiazanyl —OCH₃ —H AVK -4-thiazanyl —OCH₂CH₃—H AVL -4-thiazanyl —OCF₃ —H AVM -4-thiazanyl -tert-butyl —H AVN-4-thiazanyl -iso-propyl —H AVO -4-thiazanyl —CH₃ —CH₃ AVP -4-thiazanyl—H —H AVQ -4-thiazanyl —H —Cl AVR -4-thiazanyl —H —Br AVS -4-thiazanyl—H —F AVT -4-thiazanyl —H —CH₃ AVU -4-thiazanyl —H —CF₃ AVV -4-thiazanyl—H —OCH₃ AVW -4-thiazanyl —H —OCH₂CH₃ AVX -4-thiazanyl —H —OCF₃ AVY-4-thiazanyl —H -tert-butyl AVZ -4-thiazanyl —H -iso-propyl AWA-5-(4-chlorothiazanyl) —Cl —H AWB -5-(4-chlorothiazanyl) —Br —H AWC-5-(4-chlorothiazanyl) —F —H AWD -5-(4-chlorothiazanyl) —CH₃ —H AWE-5-(4-chlorothiazanyl) —CF₃ —H AWF -5-(4-chlorothiazanyl) —OCH₃ —H AWG-5-(4-chlorothiazanyl) —OCH₂CH₃ —H AWH -5-(4-chlorothiazanyl) —OCF₃ —HAWI -5-(4-chlorothiazanyl) -tert-butyl —H AWJ -5-(4-chlorothiazanyl)-iso-propyl —H AWK -5-(4-chlorothiazanyl) —CH₃ —CH₃ AWL-5-(4-chlorothiazanyl) —H —H AWM -5-(4-chlorothiazanyl) —H —Cl AWN-5-(4-chlorothiazanyl) —H —Br AWO -5-(4-chlorothiazanyl) —H —F AWP-5-(4-chlorothiazanyl) —H —CH₃ AWQ -5-(4-chlorothiazanyl) —H —CF₃ AWR-5-(4-chlorothiazanyl) —H —OCH₃ AWS -5-(4-chlorothiazanyl) —H —OCH₂CH₃AWT -5-(4-chlorothiazanyl) —H —OCF₃ AWU -5-(4-chlorothiazanyl) —H-tert-butyl AWV -5-(4-chlorothiazanyl) —H -iso-propyl AWW-5-(4-methylthiazanyl) —Cl —H AWX -5-(4-methylthiazanyl) —Br —H AWY-5-(4-methylthiazanyl) —F —H AWZ -5-(4-methylthiazanyl) —CH₃ —H AXA-5-(4-methylthiazanyl) —CF₃ —H AXB -5-(4-methylthiazanyl) —OCH₃ —H AXC-5-(4-methylthiazanyl) —OCH₂CH₃ —H AXD -5-(4-methylthiazanyl) —OCF₃ —HAXE -5-(4-methylthiazanyl) -tert-butyl —H AXF -5-(4-methylthiazanyl)-iso-propyl —H AXG -5-(4-methylthiazanyl) —CH₃ —CH₃ AXH-5-(4-methylthiazanyl) —H —H AXI -5-(4-methylthiazanyl) —H —Cl AXJ-5-(4-methylthiazanyl) —H —Br AXK -5-(4-methylthiazanyl) —H —F AXL-5-(4-methylthiazanyl) —H —CH₃ AXM -5-(4-methylthiazanyl) —H —CF₃ AXN-5-(4-methylthiazanyl) —H —OCH₃ AXO -5-(4-methylthiazanyl) —H —OCH₂CH₃AXP -5-(4-methylthiazanyl) —H —OCF₃ AXQ -5-(4-methylthiazanyl) —H-tert-butyl AXR -5-(4-methylthiazanyl) —H -iso-propyl

TABLE III

and pharmaceutically acceptable salts thereof, wherein: Compound Ar₁ R₈R₉ AXS (a, b, and c) -2-(3-chloropyridyl) —Cl —H AXT (a, b, and c)-2-(3-chloropyridyl) —Br —H AXU (a, b, and c) -2-(3-chloropyridyl) —F —HAXV (a, b, and c) -2-(3-chloropyridyl) —CH₃ —H AXW -2-(3-chloropyridyl)—CF₃ —H (a, b, and c) AXX (a, b, and c) -2-(3-chloropyridyl) —OCH₃ —HAXY (a, b, and c) -2-(3-chloropyridyl) —OCH₂CH₃ —H AXZ (a, b, and c)-2-(3-chloropyridyl) —OCF₃ —H AYA (a, b, and c) -2-(3-chloropyridyl)-tert-butyl —H AYB (a, b, and c) -2-(3-chloropyridyl) -iso-propyl —H AYC(a, b, and c) -2-(3-chloropyridyl) —CH₃ —CH₃ AYD (a, b, and c)-2-(3-chloropyridyl) —H —H AYE (a, b, and c) -2-(3-chloropyridyl) —H —ClAYF (a, b, and c) -2-(3-chloropyridyl) —H —Br AYG (a, b, and c)-2-(3-chloropyridyl) —H —F AYH (a, b, and c) -2-(3-chloropyridyl) —H—CH₃ AYI (a, b, and c) -2-(3-chloropyridyl) —H —CF₃ AYJ (a, b, and c)-2-(3-chloropyridyl) —H —OCH₃ AYK (a, b, and c) -2-(3-chloropyridyl) —H—OCH₂CH₃ AYL (a, b, and c) -2-(3-chloropyridyl) —H —OCF₃ AYM-2-(3-chloropyridyl) —H -tert-butyl (a, b, and c) AYN (a, b, and c)-2-(3-chloropyridyl) —H -iso-propyl AYO (a, b, and c)-2-(3-methylpyridyl) —Cl —H AYP (a, b, and c) -2-(3-methylpyridyl) —Br—H AYQ (a, b, and c) -2-(3-methylpyridyl) —F —H AYR (a, b, and c)-2-(3-methylpyridyl) —CH₃ —H AYS (a, b, and c) -2-(3-methylpyridyl) —CF₃—H AYT (a, b, and c) -2-(3-methylpyridyl) —OCH₃ —H AYU (a, b, and c)-2-(3-methylpyridyl) —OCH₂CH₃ —H AYV (a, b, and c) -2-(3-methylpyridyl)—OCF₃ —H AYW -2-(3-methylpyridyl) -tert-butyl —H (a, b, and c) AYX (a,b, and c) -2-(3-methylpyridyl) -iso-propyl —H AYY (a, b, and c)-2-(3-methylpyridyl) —CH₃ —CH₃ AYZ (a, b, and c) -2-(3-methylpyridyl) —H—H AZA (a, b, and c) -2-(3-methylpyridyl) —H —Cl AZB (a, b, and c)-2-(3-methylpyridyl) —H —Br AZC (a, b, and c) -2-(3-methylpyridyl) —H —FAZD (a, b, and c) -2-(3-methylpyridyl) —H —CH₃ AZE (a, b, and c)-2-(3-methylpyridyl) —H —CF₃ AZF (a, b, and c) -2-(3-methylpyridyl) —H—OCH₃ AZG (a, b, and c) -2-(3-methylpyridyl) —H —OCH₂CH₃ AZH (a, b, andc) -2-(3-methylpyridyl) —H —OCF₃ AZI (a, b, and c) -2-(3-methylpyridyl)—H -tert-butyl AZJ (a, b, and c) -2-(3-methylpyridyl) —H -iso-propyl AZK(a, b, and c) -2-(3-CF₃-pyridyl) —Cl —H AZL (a, b, and c)-2-(3-CF₃-pyridyl) —Br —H AZM (a, b, and c) -2-(3-CF₃-pyridyl) —F —H AZN(a, b, and c) -2-(3-CF₃-pyridyl) —CH₃ —H AZO (a, b, and c)-2-(3-CF₃-pyridyl) —CF₃ —H AZP (a, b, and c) -2-(3-CF₃-pyridyl) —OCH₃ —HAZQ (a, b, and c) -2-(3-CF₃-pyridyl) —OCH₂CH₃ —H AZR (a, b, and c)-2-(3-CF₃-pyridyl) —OCF₃ —H AZS (a, b, and c) -2-(3-CF₃-pyridyl)-tert-butyl —H AZT (a, b, and c) -2-(3-CF₃-pyridyl) -iso-propyl —H AZU(a, b, and c) -2-(3-CF₃-pyridyl) —CH₃ —CH₃ AZV (a, b, and c)-2-(3-CF₃-pyridyl) —H —H AZW -2-(3-CF₃-pyridyl) —H —Cl (a, b, and c) AZX(a, b, and c) -2-(3-CF₃-pyridyl) —H —Br AZY (a, b, and c)-2-(3-CF₃-pyridyl) —H —F AZZ (a, b, and c) -2-(3-CF₃-pyridyl) —H —CH₃BAA (a, b, and c) -2-(3-CF₃-pyridyl) —H —CF₃ BAB (a, b, and c)-2-(3-CF₃-pyridyl) —H —OCH₃ BAC (a, b, and c) -2-(3-CF₃-pyridyl) —H—OCH₂CH₃ BAD (a, b, and c) -2-(3-CF₃-pyridyl) —H —OCF₃ BAE (a, b, and c)-2-(3-CF₃-pyridyl) —H -tert-butyl BAF (a, b, and c) -2-(3-CF₃-pyridyl)—H -iso-propyl BAG (a, b, and c) -4-(5-chloropyrimidinyl) —Cl —H BAH (a,b, and c) -4-(5-chloropyrimidinyl) —Br —H BAI (a, b, and c)-4-(5-chloropyrimidinyl) —F —H BAJ (a, b, and c)-4-(5-chloropyrimidinyl) —CH₃ —H BAK (a, b, and c)-4-(5-chloropyrimidinyl) —CF₃ —H BAL (a, b, and c)-4-(5-chloropyrimidinyl) —OCH₃ —H BAM -4-(5-chloropyrimidinyl) —OCH₂CH₃—H (a, b, and c) BAN (a, b, and c) -4-(5-chloropyrimidinyl) —OCF₃ —H BAO(a, b, and c) -4-(5-chloropyrimidinyl) -tert-butyl —H BAP (a, b, and c)-4-(5-chloropyrimidinyl) -iso-propyl —H BAQ (a, b, and c)-4-(5-chloropyrimidinyl) —CH₃ —CH₃ BAR (a, b, and c)-4-(5-chloropyrimidinyl) —H —H BAS (a, b, and c)-4-(5-chloropyrimidinyl) —H —Cl BAT (a, b, and c)-4-(5-chloropyrimidinyl) —H —Br BAU (a, b, and c)-4-(5-chloropyrimidinyl) —H —F BAV (a, b, and c)-4-(5-chloropyrimidinyl) —H —CH₃ BAW -4-(5-chloropyrimidinyl) —H —CF₃(a, b, and c) BAX (a, b, and c) -4-(5-chloropyrimidinyl) —H —OCH₃ BAY(a, b, and c) -4-(5-chloropyrimidinyl) —H —OCH₂CH₃ BAZ (a, b, and c)-4-(5-chloropyrimidinyl) —H —OCF₃ BBA (a, b, and c)-4-(5-chloropyrimidinyl) —H -tert-butyl BBB (a, b, and c)-4-(5-chloropyrimidinyl) —H -iso-propyl BBC (a, b, and c)-4-(5-methylpyrimidinyl) —Cl —H BBD (a, b, and c)-4-(5-methylpyrimidinyl) —Br —H BBE (a, b, and c)-4-(5-methylpyrimidinyl) —F —H BBF (a, b, and c)-4-(5-methylpyrimidinyl) —CH₃ —H BBG (a, b, and c)-4-(5-methylpyrimidinyl) —CF₃ —H BBH (a, b, and c)-4-(5-methylpyrimidinyl) —OCH₃ —H BBI (a, b, and c)-4-(5-methylpyrimidinyl) —OCH₂CH₃ —H BBJ (a, b, and c)-4-(5-methylpyrimidinyl) —OCF₃ —H BBK (a, b, and c)-4-(5-methylpyrimidinyl) -tert-butyl —H BBL (a, b, and c)-4-(5-methylpyrimidinyl) -iso-propyl —H BBM (a, b, and c)-4-(5-methylpyrimidinyl) —CH₃ —CH₃ BBN (a, b, and c)-4-(5-methylpyrimidinyl) —H —H BBO (a, b, and c)-4-(5-methylpyrimidinyl) —H —Cl BBP (a, b, and c)-4-(5-methylpyrimidinyl) —H —Br BBQ (a, b, and c)-4-(5-methylpyrimidinyl) —H —F BBR (a, b, and c)-4-(5-methylpyrimidinyl) —H —CH₃ BBS (a, b, and c)-4-(5-methylpyrimidinyl) —H —CF₃ BBT (a, b, and c)-4-(5-methylpyrimidinyl) —H —OCH₃ BBU (a, b, and c)-4-(5-methylpyrimidinyl) —H —OCH₂CH₃ BBV (a, b, and c)-4-(5-methylpyrimidinyl) —H —OCF₃ BBW -4-(5-methylpyrimidinyl) —H-tert-butyl (a, b, and c) BBX (a, b, and c) -4-(5-methylpyrimidinyl) —H-iso-propyl BBY (a, b, and c) -2-pyrazinyl —Cl —H BBZ (a, b, and c)-2-pyrazinyl —Br —H BCA (a, b, and c) -2-pyrazinyl —F —H BCB (a, b, andc) -2-pyrazinyl —CH₃ —H BCC (a, b, and c) -2-pyrazinyl —CF₃ —H BCD (a,b, and c) -2-pyrazinyl —OCH₃ —H BCE (a, b, and c) -2-pyrazinyl —OCH₂CH₃—H BCF (a, b, and c) -2-pyrazinyl —OCF₃ —H BCG (a, b, and c)-2-pyrazinyl -tert-butyl —H BCH (a, b, and c) -2-pyrazinyl -iso-propyl—H BCI (a, b, and c) -2-pyrazinyl —CH₃ —CH₃ BCJ (a, b, and c)-2-pyrazinyl —H —H BCK (a, b, and c) -2-pyrazinyl —H —Cl BCL (a, b, andc) -2-pyrazinyl —H —Br BCM (a, b, and c) -2-pyrazinyl —H —F BCN (a, b,and c) -2-pyrazinyl —H —CH₃ BCO (a, b, and c) -2-pyrazinyl —H —CF₃ BCP(a, b, and c) -2-pyrazinyl —H —OCH₃ BCQ (a, b, and c) -2-pyrazinyl —H—OCH₂CH₃ BCR (a, b, and c) -2-pyrazinyl —H —OCF₃ BCS (a, b, and c)-2-pyrazinyl —H -tert-butyl BCT (a, b, and c) -2-pyrazinyl —H-iso-propyl BCU (a, b, and c) -2-(3-chloropyrazinyl) —Cl —H BCV (a, b,and c) -2-(3-chloropyrazinyl) —Br —H BCW -2-(3-chloropyrazinyl) —F —H(a, b, and c) BCX (a, b, and c) -2-(3-chloropyrazinyl) —CH₃ —H BCY (a,b, and c) -2-(3-chloropyrazinyl) —CF₃ —H BCZ (a, b, and c)-2-(3-chloropyrazinyl) —OCH₃ —H BDA (a, b, and c) -2-(3-chloropyrazinyl)—OCH₂CH₃ —H BDB (a, b, and c) -2-(3-chloropyrazinyl) —OCF₃ —H BDC (a, b,and c) -2-(3-chloropyrazinyl) -tert-butyl —H BDD (a, b, and c)-2-(3-chloropyrazinyl) -iso-propyl —H BDE (a, b, and c)-2-(3-chloropyrazinyl) —CH₃ —CH₃ BDF (a, b, and c)-2-(3-chloropyrazinyl) —H —H BDG (a, b, and c) -2-(3-chloropyrazinyl) —H—Cl BDH (a, b, and c) -2-(3-chloropyrazinyl) —H —Br BDI (a, b, and c)-2-(3-chloropyrazinyl) —H —F BDJ (a, b, and c) -2-(3-chloropyrazinyl) —H—CH₃ BDK (a, b, and c) -2-(3-chloropyrazinyl) —H —CF₃ BDL (a, b, and c)-2-(3-chloropyrazinyl) —H —OCH₃ BDM -2-(3-chloropyrazinyl) —H —OCH₂CH₃(a, b, and c) BDN (a, b, and c) -2-(3-chloropyrazinyl) —H —OCF₃ BDO (a,b, and c) -2-(3-chloropyrazinyl) —H -tert-butyl BDP (a, b, and c)-2-(3-chloropyrazinyl) —H -iso-propyl BDQ (a, b, and c)-2-(3-methylpyrazinyl) —Cl —H BDR (a, b, and c) -2-(3-methylpyrazinyl)—Br —H BDS (a, b, and c) -2-(3-methylpyrazinyl) —F —H BDT (a, b, and c)-2-(3-methylpyrazinyl) —CH₃ —H BDU (a, b, and c) -2-(3-methylpyrazinyl)—CF₃ —H BDV (a, b, and c) -2-(3-methylpyrazinyl) —OCH₃ —H BDW-2-(3-methylpyrazinyl) —OCH₂CH₃ —H (a, b, and c) BDX (a, b, and c)-2-(3-methylpyrazinyl) —OCF₃ —H BDY (a, b, and c) -2-(3-methylpyrazinyl)-tert-butyl —H BDZ (a, b, and c) -2-(3-methylpyrazinyl) -iso-propyl —HBEA (a, b, and c) -2-(3-methylpyrazinyl) —CH₃ —CH₃ BEB (a, b, and c)-2-(3-methylpyrazinyl) —H —H BEC (a, b, and c) -2-(3-methylpyrazinyl) —H—Cl BED (a, b, and c) -2-(3-methylpyrazinyl) —H —Br BEE (a, b, and c)-2-(3-methylpyrazinyl) —H —F BEF (a, b, and c) -2-(3-methylpyrazinyl) —H—CH₃ BEG (a, b, and c) -2-(3-methylpyrazinyl) —H —CF₃ BEH (a, b, and c)-2-(3-methylpyrazinyl) —H —OCH₃ BEI (a, b, and c) -2-(3-methylpyrazinyl)—H —OCH₂CH₃ BEJ (a, b, and c) -2-(3-methylpyrazinyl) —H —OCF₃ BEK (a, b,and c) -2-(3-methylpyrazinyl) —H -tert-butyl BEL (a, b, and c)-2-(3-methylpyrazinyl) —H -iso-propyl BEM (a, b, and c) -2-pyridazinyl—Cl —H BEN (a, b, and c) -2-pyridazinyl —Br —H BEO (a, b, and c)-2-pyridazinyl —F —H BEP (a, b, and c) -2-pyridazinyl —CH₃ —H BEQ (a, b,and c) -2-pyridazinyl —CF₃ —H BER (a, b, and c) -2-pyridazinyl —OCH₃ —HBES (a, b, and c) -2-pyridazinyl —OCH₂CH₃ —H BET (a, b, and c)-2-pyridazinyl —OCF₃ —H BEU (a, b, and c) -2-pyridazinyl -tert-butyl —HBEV (a, b, and c) -2-pyridazinyl -iso-propyl —H BEW (a, b, and c)-2-pyridazinyl —CH₃ —CH₃ BEX (a, b, and c) -2-pyridazinyl —H —H BEY (a,b, and c) -2-pyridazinyl —H —Cl BEZ (a, b, and c) -2-pyridazinyl —H —BrBFA (a, b, and c) -2-pyridazinyl —H —F BFB (a, b, and c) -2-pyridazinyl—H —CH₃ BFC (a, b, and c) -2-pyridazinyl —H —CF₃ BFD (a, b, and c)-2-pyridazinyl —H —OCH₃ BFE (a, b, and c) -2-pyridazinyl —H —OCH₂CH₃ BFF(a, b, and c) -2-pyridazinyl —H —OCF₃ BFG (a, b, and c) -2-pyridazinyl—H -tert-butyl BFH (a, b, and c) -2-pyridazinyl —H -iso-propyl BFI (a,b, and c) -3-(4-chloropyridazinyl) —Cl —H BFJ (a, b, and c)-3-(4-chloropyridazinyl) —Br —H BFK (a, b, and c)-3-(4-chloropyridazinyl) —F —H BFL (a, b, and c)-3-(4-chloropyridazinyl) —CH₃ —H BFM (a, b, and c)-3-(4-chloropyridazinyl) —CF₃ —H BFN (a, b, and c)-3-(4-chloropyridazinyl) —OCH₃ —H BFO (a, b, and c)-3-(4-chloropyridazinyl) —OCH₂CH₃ —H BFP (a, b, and c)-3-(4-chloropyridazinyl) —OCF₃ —H BFQ (a, b, and c)-3-(4-chloropyridazinyl) -tert-butyl —H BFR (a, b, and c)-3-(4-chloropyridazinyl) -iso-propyl —H BFS (a, b, and c)-3-(4-chloropyridazinyl) —CH₃ —CH₃ BFT (a, b, and c)-3-(4-chloropyridazinyl) —H —H BFU (a, b, and c)-3-(4-chloropyridazinyl) —H —Cl BFV (a, b, and c)-3-(4-chloropyridazinyl) —H —Br BFW (a, b, and c)-3-(4-chloropyridazinyl) —H —F BFX (a, b, and c)-3-(4-chloropyridazinyl) —H —CH₃ BFY (a, b, and c)-3-(4-chloropyridazinyl) —H —CF₃ BFZ (a, b, and c)-3-(4-chloropyridazinyl) —H —OCH₃ BGA (a, b, and c)-3-(4-chloropyridazinyl) —H —OCH₂CH₃ BGB (a, b, and c)-3-(4-chloropyridazinyl) —H —OCF₃ BGC (a, b, and c)-3-(4-chloropyridazinyl) —H -tert-butyl BGD (a, b, and c)-3-(4-chloropyridazinyl) —H -iso-propyl BGE (a, b, and c)-3-(4-methylpyridazinyl) —Cl —H BGF (a, b, and c)-3-(4-methylpyridazinyl) —Br —H BGG (a, b, and c)-3-(4-methylpyridazinyl) —F —H BGH (a, b, and c)-3-(4-methylpyridazinyl) —CH₃ —H BGI (a, b, and c)-3-(4-methylpyridazinyl) —CF₃ —H BGJ (a, b, and c)-3-(4-methylpyridazinyl) —OCH₃ —H BGK (a, b, and c)-3-(4-methylpyridazinyl) —OCH₂CH₃ —H BGL (a, b, and c)-3-(4-methylpyridazinyl) —OCF₃ —H BGM -3-(4-methylpyridazinyl)-tert-butyl —H (a, b, and c) BGN (a, b, and c) -3-(4-methylpyridazinyl)-iso-propyl —H BGO (a, b, and c) -3-(4-methylpyridazinyl) —CH₃ —CH₃ BGP(a, b, and c) -3-(4-methylpyridazinyl) —H —H BGQ (a, b, and c)-3-(4-methylpyridazinyl) —H —Cl BGR (a, b, and c)-3-(4-methylpyridazinyl) —H —Br BGS (a, b, and c)-3-(4-methylpyridazinyl) —H —F BGT (a, b, and c)-3-(4-methylpyridazinyl) —H —CH₃ BGU (a, b, and c)-3-(4-methylpyridazinyl) —H —CF₃ BGV (a, b, and c)-3-(4-methylpyridazinyl) —H —OCH₃ BGW -3-(4-methylpyridazinyl) —H—OCH₂CH₃ (a, b, and c) BGX (a, b, and c) -3-(4-methylpyridazinyl) —H—OCF₃ BGY (a, b, and c) -3-(4-methylpyridazinyl) —H -tert-butyl BGZ (a,b, and c) -3-(4-methylpyridazinyl) —H -iso-propyl BHA (a, b, and c)-4-thiazanyl —Cl —H BHB (a, b, and c) -4-thiazanyl —Br —H BHC (a, b, andc) -4-thiazanyl —F —H BHD (a, b, and c) -4-thiazanyl —CH₃ —H BHE (a, b,and c) -4-thiazanyl —CF₃ —H BHF (a, b, and c) -4-thiazanyl —OCH₃ —H BHG(a, b, and c) -4-thiazanyl —OCH₂CH₃ —H BHH (a, b, and c) -4-thiazanyl—OCF₃ —H BHI (a, b, and c) -4-thiazanyl -tert-butyl —H BHJ (a, b, and c)-4-thiazanyl -iso-propyl —H BHK (a, b, and c) -4-thiazanyl —CH₃ —CH₃ BHL(a, b, and c) -4-thiazanyl —H —H BHM -4-thiazanyl —H —Cl (a, b, and c)BHN (a, b, and c) -4-thiazanyl —H —Br BHO (a, b, and c) -4-thiazanyl —H—F BHP (a, b, and c) -4-thiazanyl —H —CH₃ BHQ (a, b, and c) -4-thiazanyl—H —CF₃ BHR (a, b, and c) -4-thiazanyl —H —OCH₃ BHS (a, b, and c)-4-thiazanyl —H —OCH₂CH₃ BHT (a, b, and c) -4-thiazanyl —H —OCF₃ BHU (a,b, and c) -4-thiazanyl —H -tert-butyl BHV (a, b, and c) -4-thiazanyl —H-iso-propyl BHW -5-(4-chlorothiazanyl) —Cl —H (a, b, and c) BHX (a, b,and c) -5-(4-chlorothiazanyl) —Br —H BHY (a, b, and c)-5-(4-chlorothiazanyl) —F —H BHZ (a, b, and c) -5-(4-chlorothiazanyl)—CH₃ —H BIA (a, b, and c) -5-(4-chlorothiazanyl) —CF₃ —H BIB (a, b, andc) -5-(4-chlorothiazanyl) —OCH₃ —H BIC (a, b, and c)-5-(4-chlorothiazanyl) —OCH₂CH₃ —H BID (a, b, and c)-5-(4-chlorothiazanyl) —OCF₃ —H BIE (a, b, and c) -5-(4-chlorothiazanyl)-tert-butyl —H BIF (a, b, and c) -5-(4-chlorothiazanyl) -iso-propyl —HBIG (a, b, and c) -5-(4-chlorothiazanyl) —CH₃ —CH₃ BIH (a, b, and c)-5-(4-chlorothiazanyl) —H —H BII (a, b, and c) -5-(4-chlorothiazanyl) —H—Cl BIJ (a, b, and c) -5-(4-chlorothiazanyl) —H —Br BIK (a, b, and c)-5-(4-chlorothiazanyl) —H —F BIL (a, b, and c) -5-(4-chlorothiazanyl) —H—CH₃ BIM (a, b, and c) -5-(4-chlorothiazanyl) —H —CF₃ BIN (a, b, and c)-5-(4-chlorothiazanyl) —H —OCH₃ BIO (a, b, and c) -5-(4-chlorothiazanyl)—H —OCH₂CH₃ BIP (a, b, and c) -5-(4-chlorothiazanyl) —H —OCF₃ BIQ (a, b,and c) -5-(4-chlorothiazanyl) —H -tert-butyl BIR (a, b, and c)-5-(4-chlorothiazanyl) —H -iso-propyl BIS (a, b, and c)-5-(4-methylthiazanyl) —Cl —H BIT (a, b, and c) -5-(4-methylthiazanyl)—Br —H BIU (a, b, and c) -5-(4-methylthiazanyl) —F —H BIV (a, b, and c)-5-(4-methylthiazanyl) —CH₃ —H BIW (a, b, and c) -5-(4-methylthiazanyl)—CF₃ —H BIX (a, b, and c) -5-(4-methylthiazanyl) —OCH₃ —H BIY (a, b, andc) -5-(4-methylthiazanyl) —OCH₂CH₃ —H BIZ (a, b, and c)-5-(4-methylthiazanyl) —OCF₃ —H BJA (a, b, and c) -5-(4-methylthiazanyl)-tert-butyl —H BJB (a, b, and c) -5-(4-methylthiazanyl) -iso-propyl —HBJC (a, b, and c) -5-(4-methylthiazanyl) —CH₃ —CH₃ BJD (a, b, and c)-5-(4-methylthiazanyl) —H —H BJE (a, b, and c) -5-(4-methylthiazanyl) —H—Cl BJF (a, b, and c) -5-(4-methylthiazanyl) —H —Br BJG (a, b, and c)-5-(4-methylthiazanyl) —H —F BJH (a, b, and c) -5-(4-methylthiazanyl) —H—CH₃ BJI (a, b, and c) -5-(4-methylthiazanyl) —H —CF₃ BJJ (a, b, and c)-5-(4-methylthiazanyl) —H —OCH₃ BJK (a, b, and c) -5-(4-methylthiazanyl)—H —OCH₂CH₃ BJL (a, b, and c) -5-(4-methylthiazanyl) —H —OCF₃ BJM (a, b,and c) -5-(4-methylthiazanyl) —H -tert-butyl BJN (a, b, and c)-5-(4-methylthiazanyl) —H -iso-propyl “a” means theBenzoazolylpiperazine Compound is racemic. “b” means the carbon atom ofthe piperazine ring attached to the methyl group is in the Rconfiguration. “c” means the carbon atom of the piperazine ring attachedto the methyl group is in the S configuration.

TABLE IV

and pharmaceutically acceptable salts thereof, wherein: Compound Ar₁ R₈R₉ BJO (a, b, and c) -2-(3-chloropyridyl) —Cl —H BJP (a, b, and c)-2-(3-chloropyridyl) —Br —H BJQ (a, b, and c) -2-(3-chloropyridyl) —F —HBJR (a, b, and c) -2-(3-chloropyridyl) —CH₃ —H BJS (a, b, and c)-2-(3-chloropyridyl) —CF₃ —H BJT (a, b, and c) -2-(3-chloropyridyl)—OCH3 —H BJU (a, b, and c) -2-(3-chloropyridyl) —OCH₂CH₃ —H BJV (a, b,and c) -2-(3-chloropyridyl) —OCF₃ —H BJW (a, b, and c)-2-(3-chloropyridyl) -tert-butyl —H BJX (a, b, and c)-2-(3-chloropyridyl) -iso-propyl —H BJY (a, b, and c)-2-(3-chloropyridyl) —CH₃ —CH₃ BJZ (a, b, and c) -2-(3-chloropyridyl) —H—H BKA (a, b, and c) -2-(3-chloropyridyl) —H —Cl BKB (a, b, and c)-2-(3-chloropyridyl) —H —Br BKC (a, b, and c) -2-(3-chloropyridyl) —H —FBKD (a, b, and c) -2-(3-chloropyridyl) —H —CH₃ BKE (a, b, and c)-2-(3-chloropyridyl) —H —CF₃ BKF (a, b, and c) -2-(3-chloropyridyl) —H—OCH₃ BKG (a, b, and c) -2-(3-chloropyridyl) —H —OCH₂CH₃ BKH (a, b, andc) -2-(3-chloropyridyl) —H —OCF₃ BKI (a, b, and c) -2-(3-chloropyridyl)—H -tert-butyl BKJ (a, b, and c) -2-(3-chloropyridyl) —H -iso-propyl BKK(a, b, and c) -2-(3-methylpyridyl) —Cl —H BKL (a, b, and c)-2-(3-methylpyridyl) —Br —H BKM (a, b, and c) -2-(3-methylpyridyl) —F —HBKN (a, b, and c) -2-(3-methylpyridyl) —CH₃ —H BKO (a, b, and c)-2-(3-methylpyridyl) —CF₃ —H BKP (a, b, and c) -2-(3-methylpyridyl)—OCH₃ —H BKQ (a, b, and c) -2-(3-methylpyridyl) —OCH₂CH₃ —H BKR (a, b,and c) -2-(3-methylpyridyl) —OCF₃ —H BKS (a, b, and c)-2-(3-methylpyridyl) -tert-butyl —H BKT (a, b, and c)-2-(3-methylpyridyl) -iso-propyl —H BKU (a, b, and c)-2-(3-methylpyridyl) —CH₃ —CH₃ BKV (a, b, and c) -2-(3-methylpyridyl) —H—H BKW (a, b, and c) -2-(3-methylpyridyl) —H —Cl BKX (a, b, and c)-2-(3-methylpyridyl) —H —Br BKY (a, b, and c) -2-(3-methylpyridyl) —H —FBKZ (a, b, and c) -2-(3-methylpyridyl) —H —CH₃ BLA (a, b, and c)-2-(3-methylpyridyl) —H —CF₃ BLB (a, b, and c) -2-(3-methylpyridyl) —H—OCH₃ BLC (a, b, and c) -2-(3-methylpyridyl) —H —OCH₂CH₃ BLD (a, b, andc) -2-(3-methylpyridyl) —H —OCF₃ BLE (a, b, and c) -2-(3-methylpyridyl)—H -tert-butyl BLF (a, b, and c) -2-(3-methylpyridyl) —H -iso-propyl BLG(a, b, and c) -2-(3-CF₃-pyridyl) —Cl —H BLH (a, b, and c)-2-(3-CF₃-pyridyl) —Br —H BLI (a, b, and c) -2-(3-CF₃-pyridyl) —F —H BLJ(a, b, and c) -2-(3-CF₃-pyridyl) —CH₃ —H BLK (a, b, and c)-2-(3-CF₃-pyridyl) —CF₃ —H BLL (a, b, and c) -2-(3-CF₃-pyridyl) —OCH₃ —HBLM (a, b, and c) -2-(3-CF₃-pyridyl) —OCH₂CH₃ —H BLN (a, b, and c)-2-(3-CF₃-pyridyl) —OCF₃ —H BLO (a, b, and c) -2-(3-CF₃-pyridyl)-tert-butyl —H BLP (a, b, and c) -2-(3-CF₃-pyridyl) -iso-propyl —H BLQ(a, b, and c) -2-(3-CF₃-pyridyl) —CH₃ —CH₃ BLR (a, b, and c)-2-(3-CF₃-pyridyl) —H —H BLS (a, b, and c) -2-(3-CF₃-pyridyl) —H —Cl BLT(a, b, and c) -2-(3-CF₃-pyridyl) —H —Br BLU (a, b, and c)-2-(3-CF₃-pyridyl) —H —F BLV (a, b, and c) -2-(3-CF₃-pyridyl) —H —CH₃BLW (a, b, and c) -2-(3-CF₃-pyridyl) —H —CF₃ BLX (a, b, and c)-2-(3-CF₃-pyridyl) —H —OCH₃ BLY (a, b, and c) -2-(3-CF₃-pyridyl) —H—OCH₂CH₃ BLZ (a, b, and c) -2-(3-CF₃-pyridyl) —H —OCF₃ BMA (a, b, and c)-2-(3-CF₃-pyridyl) —H -tert-butyl BMB (a, b, and c) -2-(3-CF₃-pyridyl)—H -iso-propyl BMC (a, b, and c) -4-(5-chloropyrimidinyl) —Cl —H BMD (a,b, and c) -4-(5-chloropyrimidinyl) —Br —H BME (a, b, and c)-4-(5-chloropyrimidinyl) —F —H BMF (a, b, and c)-4-(5-chloropyrimidinyl) —CH₃ —H BMG (a, b, and c)-4-(5-chloropyrimidinyl) —CF₃ —H BMH (a, b, and c)-4-(5-chloropyrimidinyl) —OCH₃ —H BMI (a, b, and c)-4-(5-chloropyrimidinyl) —OCH₂CH₃ —H BMJ (a, b, and c)-4-(5-chloropyrimidinyl) —OCF₃ —H BMK (a, b, and c)-4-(5-chloropyrimidinyl) -tert-butyl —H BML (a, b, and c)-4-(5-chloropyrimidinyl) -iso-propyl —H BMM (a, b, and c)-4-(5-chloropyrimidinyl) —CH₃ —CH₃ BMN (a, b, and c)-4-(5-chloropyrimidinyl) —H —H BMO (a, b, and c)-4-(5-chloropyrimidinyl) —H —Cl BMP (a, b, and c)-4-(5-chloropyrimidinyl) —H —Br BMQ (a, b, and c)-4-(5-chloropyrimidinyl) —H —F BMR (a, b, and c)-4-(5-chloropyrimidinyl) —H —CH₃ BMS (a, b, and c)-4-(5-chloropyrimidinyl) —H —CF₃ BMT (a, b, and c)-4-(5-chloropyrimidinyl) —H —OCH₃ BMU (a, b, and c)-4-(5-chloropyrimidinyl) —H —OCH₂CH₃ BMV (a, b, and c)-4-(5-chloropyrimidinyl) —H —OCF₃ BMW (a, b, and c)-4-(5-chloropyrimidinyl) —H -tert-butyl BMX (a, b, and c)-4-(5-chloropyrimidinyl) —H -iso-propyl BMY (a, b, and c)-4-(5-methylpyrimidinyl) —Cl —H BMZ (a, b, and c)-4-(5-methylpyrimidinyl) —Br —H BNA (a, b, and c)-4-(5-methylpyrimidinyl) —F —H BNB (a, b, and c)-4-(5-methylpyrimidinyl) —CH₃ —H BNC (a, b, and c)-4-(5-methylpyrimidinyl) —CF₃ —H BND (a, b, and c)-4-(5-methylpyrimidinyl) —OCH₃ —H BNE (a, b, and c)-4-(5-methylpyrimidinyl) —OCH₂CH₃ —H BNF (a, b, and c)-4-(5-methylpyrimidinyl) —OCF₃ —H BNG (a, b, and c)-4-(5-methylpyrimidinyl) -tert-butyl —H BNH (a, b, and c)-4-(5-methylpyrimidinyl) -iso-propyl —H BNI (a, b, and c)-4-(5-methylpyrimidinyl) —CH₃ —CH₃ BNJ (a, b, and c)-4-(5-methylpyrimidinyl) —H —H BNK (a, b, and c)-4-(5-methylpyrimidinyl) —H —Cl BNL (a, b, and c)-4-(5-methylpyrimidinyl) —H —Br BNM (a, b, and c)-4-(5-methylpyrimidinyl) —H —F BNN (a, b, and c)-4-(5-methylpyrimidinyl) —H —CH₃ BNO (a, b, and c)-4-(5-methylpyrimidinyl) —H —CF₃ BNP (a, b, and c)-4-(5-methylpyrimidinyl) —H —OCH₃ BNQ (a, b, and c)-4-(5-methylpyrimidinyl) —H —OCH₂CH₃ BNR (a, b, and c)-4-(5-methylpyrimidinyl) —H —OCF₃ BNS (a, b, and c)-4-(5-methylpyrimidinyl) —H -tert-butyl BNT (a, b, and c)-4-(5-methylpyrimidinyl) —H -iso-propyl BNU (a, b, and c) -2-pyrazinyl—Cl —H BNV (a, b, and c) -2-pyrazinyl —Br —H BNW (a, b, and c)-2-pyrazinyl —F —H BNX (a, b, and c) -2-pyrazinyl —CH₃ —H BNY (a, b, andc) -2-pyrazinyl —CF₃ —H BNZ (a, b, and c) -2-pyrazinyl —OCH₃ —H BOA (a,b, and c) -2-pyrazinyl —OCH₂CH₃ —H BOB (a, b, and c) -2-pyrazinyl —OCF₃—H BOC (a, b, and c) -2-pyrazinyl -tert-butyl —H BOD (a, b, and c)-2-pyrazinyl -iso-propyl —H BOE (a, b, and c) -2-pyrazinyl —CH₃ —CH₃ BOF(a, b, and c) -2-pyrazinyl —H —H BOG (a, b, and c) -2-pyrazinyl —H —ClBOH (a, b, and c) -2-pyrazinyl —H —Br BOI (a, b, and c) -2-pyrazinyl —H—F BOJ (a, b, and c) -2-pyrazinyl —H —CH₃ BOK (a, b, and c) -2-pyrazinyl—H —CF₃ BOL (a, b, and c) -2-pyrazinyl —H —OCH₃ BOM (a, b, and c)-2-pyrazinyl —H —OCH₂CH₃ BON (a, b, and c) -2-pyrazinyl —H —OCF₃ BOO (a,b, and c) -2-pyrazinyl —H -tert-butyl BOP (a, b, and c) -2-pyrazinyl —H-iso-propyl BOQ (a, b, and c) -2-(3-chloropyrazinyl) —Cl —H BOR (a, b,and c) -2-(3-chloropyrazinyl) —Br —H BOS (a, b, and c)-2-(3-chloropyrazinyl) —F —H BOT (a, b, and c) -2-(3-chloropyrazinyl)—CH₃ —H BOU (a, b, and c) -2-(3-chloropyrazinyl) —CF₃ —H BOV (a, b, andc) -2-(3-chloropyrazinyl) —OCH₃ —H BOW (a, b, and c)-2-(3-chloropyrazinyl) —OCH₂CH₃ —H BOX (a, b, and c)-2-(3-chloropyrazinyl) —OCF₃ —H BOY (a, b, and c) -2-(3-chloropyrazinyl)-tert-butyl —H BOZ (a, b, and c) -2-(3-chloropyrazinyl) -iso-propyl —HBPA (a, b, and c) -2-(3-chloropyrazinyl) —CH₃ —CH₃ BPB (a, b, and c)-2-(3-chloropyrazinyl) —H —H BPC (a, b, and c) -2-(3-chloropyrazinyl) —H—Cl BPD (a, b, and c) -2-(3-chloropyrazinyl) —H —Br BPE (a, b, and c)-2-(3-chloropyrazinyl) —H —F BPF (a, b, and c) -2-(3-chloropyrazinyl) —H—CH₃ BPG (a, b, and c) -2-(3-chloropyrazinyl) —H —CF₃ BPH (a, b, and c)-2-(3-chloropyrazinyl) —H —OCH₃ BPI (a, b, and c) -2-(3-chloropyrazinyl)—H —OCH₂CH₃ BPJ (a, b, and c) -2-(3-chloropyrazinyl) —H —OCF₃ BPK (a, b,and c) -2-(3-chloropyrazinyl) —H -tert-butyl BPL (a, b, and c)-2-(3-chloropyrazinyl) —H -iso-propyl BPM (a, b, and c)-2-(3-methylpyrazinyl) —Cl —H BPN (a, b, and c) -2-(3-methylpyrazinyl)—Br —H BPO (a, b, and c) -2-(3-methylpyrazinyl) —F —H BPP (a, b, and c)-2-(3-methylpyrazinyl) —CH₃ —H BPQ (a, b, and c) -2-(3-methylpyrazinyl)—CF₃ —H BPR (a, b, and c) -2-(3-methylpyrazinyl) —OCH₃ —H BPS (a, b, andc) -2-(3-methylpyrazinyl) —OCH₂CH₃ —H BPT (a, b, and c)-2-(3-methylpyrazinyl) —OCF₃ —H BPU (a, b, and c) -2-(3-methylpyrazinyl)-tert-butyl —H BPV (a, b, and c) -2-(3-methylpyrazinyl) -iso-propyl —HBPW (a, b, and c) -2-(3-methylpyrazinyl) —CH₃ —CH₃ BPX (a, b, and c)-2-(3-methylpyrazinyl) —H —H BPY (a, b, and c) -2-(3-methylpyrazinyl) —H—Cl BPZ (a, b, and c) -2-(3-methylpyrazinyl) —H —Br BQA (a, b, and c)-2-(3-methylpyrazinyl) —H —F BQB (a, b, and c) -2-(3-methylpyrazinyl) —H—CH₃ BQC (a, b, and c) -2-(3-methylpyrazinyl) —H —CF₃ BQD (a, b, and c)-2-(3-methylpyrazinyl) —H —OCH₃ BQE (a, b, and c) -2-(3-methylpyrazinyl)—H —OCH₂CH₃ BQF (a, b, and c) -2-(3-methylpyrazinyl) —H —OCF₃ BQG (a, b,and c) -2-(3-methylpyrazinyl) —H -tert-butyl BQH (a, b, and c)-2-(3-methylpyrazinyl) —H -iso-propyl BQI (a, b, and c) -2-pyridazinyl—Cl —H BQJ (a, b, and c) -2-pyridazinyl —Br —H BQK (a, b, and c)-2-pyridazinyl —F —H BQL (a, b, and c) -2-pyridazinyl —CH₃ —H BQM (a, b,and c) -2-pyridazinyl —CF₃ —H BQN (a, b, and c) -2-pyridazinyl —OCH₃ —HBQO (a, b, and c) -2-pyridazinyl —OCH₂CH₃ —H BQP (a, b, and c)-2-pyridazinyl —OCF₃ —H BQQ (a, b, and c) -2-pyridazinyl -tert-butyl —HBQR (a, b, and c) -2-pyridazinyl -iso-propyl —H BQS (a, b, and c)-2-pyridazinyl —CH₃ —CH₃ BQT (a, b, and c) -2-pyridazinyl —H —H BQU (a,b, and c) -2-pyridazinyl —H —Cl BQV (a, b, and c) -2-pyridazinyl —H —BrBQW (a, b, and c) -2-pyridazinyl —H —F BQX (a, b, and c) -2-pyridazinyl—H —CH₃ BQY (a, b, and c) -2-pyridazinyl —H —CF₃ BQZ (a, b, and c)-2-pyridazinyl —H —OCH₃ BRA (a, b, and c) -2-pyridazinyl —H —OCH₂CH₃ BRB(a, b, and c) -2-pyridazinyl —H —OCF₃ BRC (a, b, and c) -2-pyridazinyl—H -tert-butyl BRD (a, b, and c) -2-pyridazinyl —H -iso-propyl BRE (a,b, and c) -3-(4-chloropyridazinyl) —Cl —H BRF (a, b, and c)-3-(4-chloropyridazinyl) —Br —H BRG (a, b, and c)-3-(4-chloropyridazinyl) —F —H BRH (a, b, and c)-3-(4-chloropyridazinyl) —CH₃ —H BRI (a, b, and c)-3-(4-chloropyridazinyl) —CF₃ —H BRJ (a, b, and c)-3-(4-chloropyridazinyl) —OCH₃ —H BRK (a, b, and c)-3-(4-chloropyridazinyl) —OCH₂CH₃ —H BRL (a, b, and c)-3-(4-chloropyridazinyl) —OCF₃ —H BRM (a, b, and c)-3-(4-chloropyridazinyl) -tert-butyl —H BRN (a, b, and c)-3-(4-chloropyridazinyl) -iso-propyl —H BRO (a, b, and c)-3-(4-chloropyridazinyl) —CH₃ —CH₃ BRP (a, b, and c)-3-(4-chloropyridazinyl) —H —H BRQ (a, b, and c)-3-(4-chloropyridazinyl) —H —Cl BRR (a, b, and c)-3-(4-chloropyridazinyl) —H —Br BRS (a, b, and c)-3-(4-chloropyridazinyl) —H —F BRT (a, b, and c)-3-(4-chloropyridazinyl) —H —CH₃ BRU (a, b, and c)-3-(4-chloropyridazinyl) —H —CF₃ BRV (a, b, and c)-3-(4-chloropyridazinyl) —H —OCH₃ BRW (a, b, and c)-3-(4-chloropyridazinyl) —H —OCH₂CH₃ BRX (a, b, and c)-3-(4-chloropyridazinyl) —H —OCF₃ BRY (a, b, and c)-3-(4-chloropyridazinyl) —H -tert-butyl BRZ (a, b, and c)-3-(4-chloropyridazinyl) —H -iso-propyl BSA (a, b, and c)-3-(4-methylpyridazinyl) —Cl —H BSB (a, b, and c)-3-(4-methylpyridazinyl) —Br —H BSC (a, b, and c)-3-(4-methylpyridazinyl) —F —H BSD (a, b, and c)-3-(4-methylpyridazinyl) —CH₃ —H BSE (a, b, and c)-3-(4-methylpyridazinyl) —CF₃ —H BSF (a, b, and c)-3-(4-methylpyridazinyl) —OCH₃ —H BSG (a, b, and c)-3-(4-methylpyridazinyl) —OCH₂CH₃ —H BSH (a, b, and c)-3-(4-methylpyridazinyl) —OCF₃ —H BSI (a, b, and c)-3-(4-methylpyridazinyl) -tert-butyl —H BSJ (a, b, and c)-3-(4-methylpyridazinyl) -iso-propyl —H BSK (a, b, and c)-3-(4-methylpyridazinyl) —CH₃ —CH₃ BSL (a, b, and c)-3-(4-methylpyridazinyl) —H —H BSM (a, b, and c)-3-(4-methylpyridazinyl) —H —Cl BSN (a, b, and c)-3-(4-methylpyridazinyl) —H —Br BSO (a, b, and c)-3-(4-methylpyridazinyl) —H —F BSP (a, b, and c)-3-(4-methylpyridazinyl) —H —CH₃ BSQ (a, b, and c)-3-(4-methylpyridazinyl) —H —CF₃ BSR (a, b, and c)-3-(4-methylpyridazinyl) —H —OCH₃ BSS (a, b, and c)-3-(4-methylpyridazinyl) —H —OCH₂CH₃ BST (a, b, and c)-3-(4-methylpyridazinyl) —H —OCF₃ BSU (a, b, and c)-3-(4-methylpyridazinyl) —H -tert-butyl BSV (a, b, and c)-3-(4-methylpyridazinyl) —H -iso-propyl BSW (a, b, and c) -4-thiazanyl—Cl —H BSX (a, b, and c) -4-thiazanyl —Br —H BSY (a, b, and c)-4-thiazanyl —F —H BSZ (a, b, and c) -4-thiazanyl —CH₃ —H BTA (a, b, andc) -4-thiazanyl —CF₃ —H BTB (a, b, and c) -4-thiazanyl —OCH₃ —H BTC (a,b, and c) -4-thiazanyl —OCH₂CH₃ —H BTD (a, b, and c) -4-thiazanyl —OCF₃—H BTE (a, b, and c) -4-thiazanyl -tert-butyl —H BTF (a, b, and c)-4-thiazanyl -iso-propyl —H BTG (a, b, and c) -4-thiazanyl —CH₃ —CH₃ BTH(a, b, and c) -4-thiazanyl —H —H BTI (a, b, and c) -4-thiazanyl —H —ClBTJ (a, b, and c) -4-thiazanyl —H —Br BTK (a, b, and c) -4-thiazanyl —H—F BTL (a, b, and c) -4-thiazanyl —H —CH₃ BTM (a, b, and c) -4-thiazanyl—H —CF₃ BTN (a, b, and c) -4-thiazanyl —H —OCH₃ BTO (a, b, and c)-4-thiazanyl —H —OCH₂CH₃ BTP (a, b, and c) -4-thiazanyl —H —OCF₃ BTQ (a,b, and c) -4-thiazanyl —H -tert-butyl BTR (a, b, and c) -4-thiazanyl —H-iso-propyl BTS (a, b, and c) -5-(4-chlorothiazanyl) —Cl —H BTT (a, b,and c) -5-(4-chlorothiazanyl) —Br —H BTU (a, b, and c)-5-(4-chlorothiazanyl) —F —H BTV (a, b, and c) -5-(4-chlorothiazanyl)—CH₃ —H BTW (a, b, and c) -5-(4-chlorothiazanyl) —CF₃ —H BTX (a, b, andc) -5-(4-chlorothiazanyl) —OCH₃ —H BTY (a, b, and c)-5-(4-chlorothiazanyl) —OCH₂CH₃ —H BTZ (a, b, and c)-5-(4-chlorothiazanyl) —OCF₃ —H BUA (a, b, and c) -5-(4-chlorothiazanyl)-tert-butyl —H BUB (a, b, and c) -5-(4-chlorothiazanyl) -iso-propyl —HBUC (a, b, and c) -5-(4-chlorothiazanyl) —CH₃ —CH₃ BUD (a, b, and c)-5-(4-chlorothiazanyl) —H —H BUE (a, b, and c) -5-(4-chlorothiazanyl) —H—Cl BUF (a, b, and c) -5-(4-chlorothiazanyl) —H —Br BUG (a, b, and c)-5-(4-chlorothiazanyl) —H —F BUH (a, b, and c) -5-(4-chlorothiazanyl) —H—CH₃ BUI (a, b, and c) -5-(4-chlorothiazanyl) —H —CF₃ BUJ (a, b, and c)-5-(4-chlorothiazanyl) —H —OCH₃ BUK (a, b, and c) -5-(4-chlorothiazanyl)—H —OCH₂CH₃ BUL (a, b, and c) -5-(4-chlorothiazanyl) —H —OCF₃ BUM (a, b,and c) -5-(4-chlorothiazanyl) —H -tert-butyl BUN (a, b, and c)-5-(4-chlorothiazanyl) —H -iso-propyl BUO (a, b, and c)-5-(4-methylthiazanyl) —Cl —H BUP (a, b, and c) -5-(4-methylthiazanyl)—Br —H BUQ (a, b, and c) -5-(4-methylthiazanyl) —F —H BUR (a, b, and c)-5-(4-methylthiazanyl) —CH₃ —H BUS (a, b, and c) -5-(4-methylthiazanyl)—CF₃ —H BUT (a, b, and c) -5-(4-methylthiazanyl) —OCH₃ —H BUU (a, b, andc) -5-(4-methylthiazanyl) —OCH₂CH₃ —H BUV (a, b, and c)-5-(4-methylthiazanyl) —OCF₃ —H BUW (a, b, and c) -5-(4-methylthiazanyl)-tert-butyl —H BUX (a, b, and c) -5-(4-methylthiazanyl) -iso-propyl —HBUY (a, b, and c) -5-(4-methylthiazanyl) —CH₃ —CH₃ BUZ (a, b, and c)-5-(4-methylthiazanyl) —H —H BVA (a, b, and c) -5-(4-methylthiazanyl) —H—Cl BVB (a, b, and c) -5-(4-methylthiazanyl) —H —Br BVC (a, b, and c)-5-(4-methylthiazanyl) —H —F BVD (a, b, and c) -5-(4-methylthiazanyl) —H—CH₃ BVE (a, b, and c) -5-(4-methylthiazanyl) —H —CF₃ BVF (a, b, and c)-5-(4-methylthiazanyl) —H —OCH₃ BVG (a, b, and c) -5-(4-methylthiazanyl)—H —OCH₂CH₃ BVH (a, b, and c) -5-(4-methylthiazanyl) —H —OCF₃ BVI (a, b,and c) -5-(4-methylthiazanyl) —H -tert-butyl BVJ (a, b, and c)-5-(4-methylthiazanyl) —H -iso-propyl “a” means theBenzoazolylpiperazine Compound is racemic. “b” means the carbon atom ofthe piperazine ring attached to the methyl group is in the Rconfiguration. “c” means the carbon atom of the piperazine ring attachedto the methyl group is in the S configuration.

TABLE V

and pharmaceutically acceptable salts thereof, wherein: Compound AR₁ R₈R₉ BVK -2-pyridazinyl —Cl —H BVL -2-pyridazinyl —Br —H BVM-2-pyridazinyl —F —H BVN -2-pyridazinyl —CH₃ —H BVO -2-pyridazinyl —CF₃—H BVP -2-pyridazinyl —OCH₃ —H BVQ -2-pyridazinyl —OCH₂CH₃ —H BVR-2-pyridazinyl —OCF₃ —H BVS -2-pyridazinyl -tert-butyl —H BVT-2-pyridazinyl -iso-propyl —H BVU -2-pyridazinyl —CH₃ —CH₃ BVV-2-pyridazinyl —H —H BVW -2-pyridazinyl —H —Cl BVX -2-pyridazinyl —H —BrBVY -2-pyridazinyl —H —F BVZ -2-pyridazinyl —H —CH₃ BWA -2-pyridazinyl—H —CF₃ BWB -2-pyridazinyl —H —OCH₃ BWC -2-pyridazinyl —H —OCH₂CH₃ BWD-2-pyridazinyl —H —OCF₃ BWE -2-pyridazinyl —H -tert-butyl BWF-2-pyridazinyl —H -iso-propyl BWG -3-(4-chloropyridazinyl) —Cl —H BWH-3-(4-chloropyridazinyl) —Br —H BWI -3-(4-chloropyridazinyl) —F —H BWJ-3-(4-chloropyridazinyl) —CH₃ —H BWK -3-(4-chloropyridazinyl) —CF₃ —HBWL -3-(4-chloropyridazinyl) —OCH₃ —H BWM -3-(4-chloropyridazinyl)—OCH₂CH₃ —H BWN -3-(4-chloropyridazinyl) —OCF₃ —H BWO-3-(4-chloropyridazinyl) -tert-butyl —H BWP -3-(4-chloropyridazinyl)-iso-propyl —H BWQ -3-(4-chloropyridazinyl) —CH₃ —CH₃ BWR-3-(4-chloropyridazinyl) —H —H BWS -3-(4-chloropyridazinyl) —H —Cl BWT-3-(4-chloropyridazinyl) —H —Br BWU -3-(4-chloropyridazinyl) —H —F BWV-3-(4-chloropyridazinyl) —H —CH₃ BWW -3-(4-chloropyridazinyl) —H —CF₃BWX -3-(4-chloropyridazinyl) —H —OCH₃ BWY -3-(4-chloropyridazinyl) —H—OCH₂CH₃ BWZ -3-(4-chloropyridazinyl) —H —OCF₃ BXA-3-(4-chloropyridazinyl) —H -tert-butyl BXB -3-(4-chloropyridazinyl) —H-iso-propyl BXC -3-(4-methylpyridazinyl) —Cl —H BXD-3-(4-methylpyridazinyl) —Br —H BXE -3-(4-methylpyridazinyl) —F —H BXF-3-(4-methylpyridazinyl) —CH₃ —H BXG -3-(4-methylpyridazinyl) —CF₃ —HBXH -3-(4-methylpyridazinyl) —OCH₃ —H BXI -3-(4-methylpyridazinyl)—OCH₂CH₃ —H BXJ -3-(4-methylpyridazinyl) —OCF₃ —H BXK-3-(4-methylpyridazinyl) -tert-butyl —H BXL -3-(4-methylpyridazinyl)-iso-propyl —H BXM -3-(4-methylpyridazinyl) —CH₃ —CH₃ BXN-3-(4-methylpyridazinyl) —H —H BXO -3-(4-methylpyridazinyl) —H —Cl BXP-3-(4-methylpyridazinyl) —H —Br BXQ -3-(4-methylpyridazinyl) —H —F BXR-3-(4-methylpyridazinyl) —H —CH₃ BXS -3-(4-methylpyridazinyl) —H —CF₃BXT -3-(4-methylpyridazinyl) —H —OCH₃ BXU -3-(4-methylpyridazinyl) —H—OCH₂CH₃ BXV -3-(4-methylpyridazinyl) —H —OCF₃ BXW-3-(4-methylpyridazinyl) —H -tert-butyl BXX -3-(4-methylpyridazinyl) —H-iso-propyl BXY -4-thiazanyl —Cl —H BXZ -4-thiazanyl —Br —H BYA-4-thiazanyl —F —H BYB -4-thiazanyl —CH₃ —H BYC -4-thiazanyl —CF₃ —H BYD-4-thiazanyl —OCH₃ —H BYE -4-thiazanyl —OCH₂CH₃ —H BYF -4-thiazanyl—OCF₃ —H BYG -4-thiazanyl -tert-butyl —H BYH -4-thiazanyl -iso-propyl —HBYL -4-thiazanyl —CH₃ —CH₃ BYJ -4-thiazanyl —H —H BYK -4-thiazanyl —H—Cl BYL -4-thiazanyl —H —Br BYM -4-thiazanyl —H —F BYN -4-thiazanyl —H—CH₃ BYO -4-thiazanyl —H —CF₃ BYP -4-thiazanyl —H —OCH₃ BYQ -4-thiazanyl—H —OCH₂CH₃ BYR -4-thiazanyl —H —OCF₃ BYS -4-thiazanyl —H -tert-butylBYT -4-thiazanyl —H -iso-propyl BYU -5-(4-chlorothiazanyl) —Cl —H BYV-5-(4-chlorothiazanyl) —Br —H BYW -5-(4-chlorothiazanyl) —F —H BYX-5-(4-chlorothiazanyl) —CH₃ —H BYY -5-(4-chlorothiazanyl) —CF₃ —H BYZ-5-(4-chlorothiazanyl) —OCH₃ —H BZA -5-(4-chlorothiazanyl) —OCH₂CH₃ —HBZB -5-(4-chlorothiazanyl) —OCF₃ —H BZC -5-(4-chlorothiazanyl)-tert-butyl —H BZD -5-(4-chlorothiazanyl) -iso-propyl —H BZE-5-(4-chlorothiazanyl) —CH₃ —CH₃ BZF -5-(4-chlorothiazanyl) —H —H BZG-5-(4-chlorothiazanyl) —H —Cl BZH -5-(4-chlorothiazanyl) —H —Br BZI-5-(4-chlorothiazanyl) —H —F BZJ -5-(4-chlorothiazanyl) —H —CH₃ BZK-5-(4-chlorothiazanyl) —H —CF₃ BZL -5-(4-chlorothiazanyl) —H —OCH₃ BZM-5-(4-chlorothiazanyl) —H —OCH₂CH₃ BZN -5-(4-chlorothiazanyl) —H —OCF₃BZO -5-(4-chlorothiazanyl) —H -tert-butyl BZP -5-(4-chlorothiazanyl) —H-iso-propyl BZQ -5-(4-methylthiazanyl) —Cl —H BZR -5-(4-methylthiazanyl)—Br —H BZS -5-(4-methylthiazanyl) —F —H BZT -5-(4-methylthiazanyl) —CH₃—H BZU -5-(4-methylthiazanyl) —CF₃ —H BZV -5-(4-methylthiazanyl) —OCH₃—H BZW -5-(4-methylthiazanyl) —OCH₂CH₃ —H BZX -5-(4-methylthiazanyl)—OCF₃ —H BZY -5-(4-methylthiazanyl) -tert-butyl —H BZZ-5-(4-methylthiazanyl) -iso-propyl —H CAA -5-(4-methylthiazanyl) —CH₃—CH₃ CAB -5-(4-methylthiazanyl) —H —H CAC -5-(4-methylthiazanyl) —H —ClCAD -5-(4-methylthiazanyl) —H —Br CAE -5-(4-methylthiazanyl) —H —F CAF-5-(4-methylthiazanyl) —H —CH₃ CAG -5-(4-methylthiazanyl) —H —CF₃ CAH-5-(4-methylthiazanyl) —H —OCH₃ CAI -5-(4-methylthia.zanyl) —H —OCH₂CH₃CAJ -5-(4-methylthiazanyl) —H —OCF₃ CAK -5-(4-methylthiazanyl) —H-tert-butyl CAL -5-(4-methyltbiazanyl) —H -iso-propyl

TABLE VI

and pharmaceutically acceptable salts thereof, wherein: Compound Ar₁ R₈R₉ CAM -2-(3-chloropyridyl) —Cl —H CAN -2-(3-chloropyridyl) —Br —H CAO-2-(3-chloropyridyl) —F —H CAP -2-(3-chloropyridyl) —CH₃ —H CAQ-2-(3-chloropyridyl) —CF₃ —H CAR -2-(3-chloropyridyl) —OCH₃ —H CAS-2-(3-chloropyridyl) —CH₂CH₃ —H CAT -2-(3-chloropyridyl) —OCF₃ —H CAU-2-(3-chloropyridyl) -tert-butyl —H CAV -2-(3-chloropyridyl) -iso-propyl—H CAW -2-(3-chloropyridyl) —CH₃ —CH₃ CAX -2-(3-chloropyridyl) —H —H CAY-2-(3-chloropyridyl) —H —Cl CAZ -2-(3-chloropyridyl) —H —Br CBA-2-(3-chloropyridyl) —H —F CBB -2-(3-chloropyridyl) —H —CH₃ CBC-2-(3-chloropyridyl) —H —CF₃ CBD -2-(3-chloropyridyl) —H —OCH₃ CBE-2-(3-chloropyridyl) —H —CH₂CH₃ CBF -2-(3-chloropyridyl) —H —OCF₃ CBG-2-(3-chloropyridyl) —H -tert-butyl CBH -2-(3-chloropyridyl) —H-iso-propyl CBI -2-(3-methylpyridyl) —Cl —H CBJ -2-(3-methylpyridyl) —Br—H CBK -2-(3-methylpyridyl) —F —H CBL -2-(3-methylpyridyl) —CH₃ —H CBM-2-(3-methylpyridyl) —CF₃ —H CBN -2-(3-methylpyridyl) —OCH₃ —H CBO-2-(3-methylpyridyl) —CH₂CH₃ —H CBP -2-(3-methylpyridyl) —OCF₃ —H CBQ-2-(3-methylpyridyl) -tert-butyl —H CBR -2-(3-methylpyridyl) -iso-propyl—H CBS -2-(3-methylpyridyl) —CH₃ —CH₃ CBT -2-(3-methylpyridyl) —H —H CBU-2-(3-methylpyridyl) —H —Cl CBV -2-(3-methylpyridyl) —H —Br CBW-2-(3-methylpyridyl) —H —F CBX -2-(3-methylpyridyl) —H —CH₃ CBY-2-(3-methylpyridyl) —H —CF₃ CBZ -2-(3-methylpyridyl) —H —OCH₃ CCA-2-(3-methylpyridyl) —H —CH₂CH₃ CCB -2-(3-methylpyridyl) —H —OCF₃ CCC-2-(3-methylpyridyl) —H -tert-butyl CCD -2-(3-methylpyridyl) —H-iso-propyl CCE -2-(3-CF₃-pyridyl) —Cl —H CCF -2-(3-CF₃-pyridyl) —Br —HCCG -2-(3-CF₃-pyridyl) —F —H CCH -2-(3-CF₃-pyridyl) —CH₃ —H CCI-2-(3-CF₃-pyridyl) —CF₃ —H CCJ -2-(3-CF₃-pyridyl) —OCH₃ —H CCK-2-(3-CF₃-pyridyl) —CH₂CH₃ —H CCL -2-(3-CF₃-pyridyl) —OCF₃ —H CCM-2-(3-CF₃-pyridyl) -tert-butyl —H CCN -2-(3-CF₃-pyridyl) -iso-propyl —HCCO -2-(3-CF₃-pyridyl) —CH₃ —CH₃ CCP -2-(3-CF₃-pyridyl) —H —H CCQ-2-(3-CF₃-pyridyl) —H —Cl CCR -2-(3-CF₃-pyridyl) —H —Br CCS-2-(3-CF₃-pyridyl) —H —F CCT -2-(3-CF₃-pyridyl) —H —CH₃ CCU-2-(3-CF₃-pyridyl) —H —CF₃ CCV -2-(3-CF₃-pyridyl) —H —OCH₃ CCW-2-(3-CF₃-pyridyl) —H —CH₂CH₃ CCX -2-(3-CF₃-pyridyl) —H —OCF₃ CCY-2-(3-CF₃-pyridyl) —H -tert-butyl CCZ -2-(3-CF₃-pyridyl) —H -iso-propylCDA -4-(5-chloropyrimidinyl) —Cl —H CDB -4-(5-chloropyrimidinyl) —Br —HCDC -4-(5-chloropyrimidinyl) —F —H CDD -4-(5-chloropyrimidinyl) —CH₃ —HCDE -4-(5-chloropyrimidinyl) —CF₃ —H CDF -4-(5-chloropyrimidinyl) —OCH₃—H CDG -4-(5-chloropyrimidinyl) —CH₂CH₃ —H CDH -4-(5-chloropyrimidinyl)—OCF₃ —H CDI -4-(5-chloropyrimidinyl) -tert-butyl —H CDJ-4-(5-chloropyrimidinyl) -iso-propyl —H CDK -4-(5-chloropyrimidinyl)—CH₃ —CH₃ CDL -4-(5-chloropyrimidinyl) —H —H CDM-4-(5-chloropyrimidinyl) —H —Cl CDN -4-(5-chloropyrimidinyl) —H —Br CDO-4-(5-chloropyrimidinyl) —H —F CDP -4-(5-chloropyrimidinyl) —H —CH₃ CDQ-4-(5-chloropyrimidinyl) —H —CF₃ CDR -4-(5-chloropyrimidinyl) —H —OCH₃CDS -4-(5-chloropyrimidinyl) —H —CH₂CH₃ CDT -4-(5-chloropyrimidinyl) —H—OCF₃ CDU -4-(5-chloropyrimidinyl) —H -tert-butyl CDV-4-(5-chloropyrimidinyl) —H -iso-propyl CDW -4-(5-methylpyrimidinyl) —Cl—H CDX -4-(5-methylpyrimidinyl) —Br —H CDY -4-(5-methylpyrimidinyl) —F—H CDZ -4-(5-methylpyrimidinyl) —CH₃ —H CEA -4-(5-methylpyrimidinyl)—CF₃ —H CEB -4-(5-methylpyrimidinyl) —OCH₃ —H CEC-4-(5-methylpyrimidinyl) —CH₂CH₃ —H CED -4-(5-methylpyrimidinyl) —OCF₃—H CEE -4-(5-methylpyrimidinyl) -tert-butyl —H CEF-4-(5-methylpyrimidinyl) -iso-propyl —H CEG -4-(5-methylpyrimidinyl)—CH₃ —CH₃ CEH -4-(5-methylpyrimidinyl) —H —H CEI-4-(5-methylpyrimidinyl) —H —Cl CEJ -4-(5-methylpyrimidinyl) —H —Br CEK-4-(5-methylpyrimidinyl) —H —F CEL -4-(5-methylpyrimidinyl) —H —CH₃ CEM-4-(5-methylpyrimidinyl) —H —CF₃ CEN -4-(5-methylpyrimidinyl) —H —OCH₃CEO -4-(5-methylpyrimidinyl) —H —CH₂CH₃ CEP -4-(5-methylpyrimidinyl) —H—OCF₃ CEQ -4-(5-methylpyrimidinyl) —H -tert-butyl CER-4-(5-methylpyrimidinyl) —H -iso-propyl CES -2-pyrazinyl —Cl —H CET-2-pyrazinyl —Br —H CEU -2-pyrazinyl —F —H CEV -2-pyrazinyl —CH₃ —H CEW-2-pyrazinyl —CF₃ —H CEX -2-pyrazinyl —OCH₃ —H CEY -2-pyrazinyl —CH₂CH₃—H CEZ -2-pyrazinyl —OCF₃ —H CFA -2-pyrazinyl -tert-butyl —H CFB-2-pyrazinyl -iso-propyl —H CFC -2-pyrazinyl —CH₃ —CH₃ CFD -2-pyrazinyl—H —H CFE -2-pyrazinyl —H —Cl CFF -2-pyrazinyl —H —Br CFG -2-pyrazinyl—H —F CFH -2-pyrazinyl —H —CH₃ CFI -2-pyrazinyl —H —CF₃ CFJ -2-pyrazinyl—H —OCH₃ CFK -2-pyrazinyl —H —CH₂CH₃ CFL -2-pyrazinyl —H —OCF₃ CFM-2-pyrazinyl —H -tert-butyl CFN -2-pyrazinyl —H -iso-propyl CFO-2-(3-chloropyrazinyl) —Cl —H CFP -2-(3-chloropyrazinyl) —Br —H CFQ-2-(3-chloropyrazinyl) —F —H CFR -2-(3-chloropyrazinyl) —CH₃ —H CFS-2-(3-chloropyrazinyl) —CF₃ —H CFT -2-(3-chloropyrazinyl) —OCH₃ —H CFU-2-(3-chloropyrazinyl) —CH₂CH₃ —H CFV -2-(3-chloropyrazinyl) —OCF₃ —HCFW -2-(3-chloropyrazinyl) -tert-butyl —H CFX -2-(3-chloropyrazinyl)-iso-propyl —H CFY -2-(3-chloropyrazinyl) —CH₃ —CH₃ CFZ-2-(3-chloropyrazinyl) —H —H CGA -2-(3-chloropyrazinyl) —H —Cl CGB-2-(3-chloropyrazinyl) —H —Br CGC -2-(3-chloropyrazinyl) —H —F CGD-2-(3-chloropyrazinyl) —H —CH₃ CGE -2-(3-chloropyrazinyl) —H —CF₃ CGF-2-(3-chloropyrazinyl) —H —OCH₃ CGG -2-(3-chloropyrazinyl) —H —CH₂CH₃CGH -2-(3-chloropyrazinyl) —H —OCF₃ CGI -2-(3-chloropyrazinyl) —H-tert-butyl CGJ -2-(3-chloropyrazinyl) —H -iso-propyl CGK-2-(3-methylpyrazinyl) —Cl —H CGL -2-(3-methylpyrazinyl) —Br —H CGM-2-(3-methylpyrazinyl) —F —H CGN -2-(3-methylpyrazinyl) —CH₃ —H CGO-2-(3-methylpyrazinyl) —CF₃ —H CGP -2-(3-methylpyrazinyl) —OCH₃ —H CGQ-2-(3-methylpyrazinyl) —CH₂CH₃ —H CGR -2-(3-methylpyrazinyl) —OCF₃ —HCGS -2-(3-methylpyrazinyl) -tert-butyl —H CGT -2-(3-methylpyrazinyl)-iso-propyl —H CGU -2-(3-methylpyrazinyl) —CH₃ —CH₃ CGV-2-(3-methylpyrazinyl) —H —H CGW -2-(3-methylpyrazinyl) —H —Cl CGX-2-(3-methylpyrazinyl) —H —Br CGY -2-(3-methylpyrazinyl) —H —F CGZ-2-(3-methylpyrazinyl) —H —CH₃ CHA -2-(3-methylpyrazinyl) —H —CF₃ CHB-2-(3-methylpyrazinyl) —H —OCH₃ CHC -2-(3-methylpyrazinyl) —H —CH₂CH₃CHD -2-(3-methylpyrazinyl) —H —OCF₃ CHE -2-(3-methylpyrazinyl) —H-tert-butyl CHF -2-(3-methylpyrazinyl) —H -iso-propyl CHG -2-pyridazinyl—Cl —H CHH -2-pyridazinyl —Br —H CHI -2-pyridazinyl —F —H CHJ-2-pyridazinyl —CH₃ —H CHK -2-pyridazinyl —CF₃ —H CHL -2-pyridazinyl—OCH₃ —H CHM -2-pyridazinyl —CH₂CH₃ —H CHN -2-pyridazinyl —OCF₃ —H CHO-2-pyridazinyl -tert-butyl —H CHP -2-pyridazinyl -iso-propyl —H CHQ-2-pyridazinyl —CH₃ —CH₃ CHR -2-pyridazinyl —H —H CHS -2-pyridazinyl —H—Cl CHT -2-pyridazinyl —H —Br CHU -2-pyridazinyl —H —F CHV-2-pyridazinyl —H —CH₃ CHW -2-pyridazinyl —H —CF₃ CHX -2-pyridazinyl —H—OCH₃ CHY -2-pyridazinyl —H —CH₂CH₃ CHZ -2-pyridazinyl —H —OCF₃ CIA-2-pyridazinyl —H -tert-butyl CIB -2-pyridazinyl —H -iso-propyl CIC-3-(4-chloropyridazinyl) —Cl —H CID -3-(4-chloropyridazinyl) —Br —H CIE-3-(4-chloropyridazinyl) —F —H CLF -3-(4-chloropyridazinyl) —CH₃ —H CIG-3-(4-chloropyridazinyl) —CF₃ —H CIH -3-(4-chloropyridazinyl) —OCH₃ —HCII -3-(4-chloropyridazinyl) —CH₂CH₃ —H CIJ -3-(4-chloropyridazinyl)—OCF₃ —H CIK -3-(4-chloropyridazinyl) -tert-butyl —H CIL-3-(4-chloropyridazinyl) -iso-propyl —H CIM -3-(4-chloropyridazinyl)—CH₃ —CH₃ CIN -3-(4-chloropyridazinyl) —H —H CIO-3-(4-chloropyridazinyl) —H —Cl CIP -3-(4-chloropyridazinyl) —H —Br CIQ-3-(4-chloropyridazinyl) —H —F CIR -3-(4-chloropyridazinyl) —H —CH₃ CIS-3-(4-chloropyridazinyl) —H —CF₃ CIT -3-(4-chloropyridazinyl) —H —OCH₃CIU -3-(4-chloropyridazinyl) —H —CH₂CH₃ CIV -3-(4-chloropyridazinyl) —H—OCF₃ CIW -3-(4-chloropyridazinyl) —H -tert-butyl CIX-3-(4-chloropyridazinyl) —H -iso-propyl CIY -3-(4-methylpyridazinyl) —Cl—H CIZ -3-(4-methylpyridazinyl) —Br —H CJA -3-(4-methylpyridazinyl) —F—H CJB -3-(4-methylpyridazinyl) —CH₃ —H CJC -3-(4-methylpyridazinyl)—CF₃ —H CJD -3-(4-methylpyridazinyl) —OCH₃ —H CJE-3-(4-methylpyridazinyl) —CH₂CH₃ —H CJF -3-(4-methylpyridazinyl) —OCF₃—H CJG -3-(4-methylpyridazinyl) -tert-butyl —H CJH-3-(4-methylpyridazinyl) -iso-propyl —H CJI -3-(4-methylpyridazinyl)—CH₃ —CH₃ CJJ -3-(4-methylpyridazinyl) —H —H CJK-3-(4-methylpyridazinyl) —H —Cl CJL -3-(4-methylpyridazinyl) —H —Br CJM-3-(4-methylpyridazinyl) —H —F CJN -3-(4-methylpyridazinyl) —H —CH₃ CJO-3-(4-methylpyridazinyl) —H —CF₃ CJP -3-(4-methylpyridazinyl) —H —OCH₃CJQ -3-(4-methylpyridazinyl) —H —CH₂CH₃ CJR -3-(4-methylpyridazinyl) —H—OCF₃ CJS -3-(4-methylpyridazinyl) —H -tert-butyl CJT-3-(4-methylpyridazinyl) —H -iso-propyl CJU -4-thiazanyl —Cl —H CJV-4-thiazanyl —Br —H CJW -4-thiazanyl —F —H CJX -4-thiazanyl —CH₃ —H CJY-4-thiazanyl —CF₃ —H CJZ -4-thiazanyl —OCH₃ —H CKA -4-thiazanyl —CH₂CH₃—H CKB -4-thiazanyl —OCF₃ —H CKC -4-thiazanyl -tert-butyl —H CKD-4-thiazanyl -iso-propyl —H CKE -4-thiazanyl —CH₃ —CH₃ CKF -4-thiazanyl—H —H CKG -4-thiazanyl —H —Cl CKH -4-thiazanyl —H —Br CKI -4-thiazanyl—H —F CKJ -4-thiazanyl —H —CH₃ CKK -4-thiazanyl —H —CF₃ CKL -4-thiazanyl—H —OCH₃ CKM -4-thiazanyl —H —CH₂CH₃ CKN -4-thiazanyl —H —OCF₃ CKO-4-thiazanyl —H -tert-butyl CKP -4-thiazanyl —H -iso-propyl CKQ-5-(4-chlorothiazanyl) —Cl —H CKR -5-(4-chlorothiazanyl) —Br —H CKS-5-(4-chlorothiazanyl) —F —H CKT -5-(4-chlorothiazanyl) —CH₃ —H CKU-5-(4-chlorothiazanyl) —CF₃ —H CKV -5-(4-chlorothiazanyl) —OCH_(3 —H)CKW -5-(4-chlorothiazanyl) —CH₂CH₃ —H CKX -5-(4-chlorothiazanyl)—OCF_(3 —H) CKY -5-(4-chlorothiazanyl) -tert-butyl —H CKZ-5-(4-chlorothiazanyl) -iso-propyl —H CLA -5-(4-chlorothiazanyl) —CH₃—CH₃ CLB -5-(4-chlorothiazanyl) —H —H CLC -5-(4-chlorothiazanyl) —H —ClCLD -5-(4-chlorothiazanyl) —H —Br CLE -5-(4-chlorothiazanyl) —H —F CLF-5-(4-chlorothiazanyl) —H —CH₃ CLG -5-(4-chlorothiazanyl) —H —CF₃ CLH-5-(4-chlorothiazanyl) —H —OCH₃ CLI -5-(4-chlorothiazanyl) —H —CH₂CH₃CLJ -5-(4-chlorothiazanyl) —H —OCF₃ CLK -5-(4-chlorotbiazanyl) —H-tert-butyl CLL -5-(4-chlorothiazanyl) —H -iso-propyl CLM-5-(4-methylthiazanyl) —Cl —H CLN -5-(4-methylthiazanyl) —Br —H CLO-5-(4-methylthiazanyl) —F —H CLP -5-(4-methylthiazanyl) —CH₃ —H CLQ-5-(4-methylthiazanyl) —CF₃ —H CLR -5-(4-methylthiazanyl) —OCH₃ —H CLS-5-(4-methylthiazanyl) —CH₂CH₃ —H CLT -5-(4-methylthiazanyl) —OCF₃ —HCLU -5-(4-methylthiazanyl) -tert-butyl —H CLV -5-(4-methylthiazanyl)-iso-propyl —H CLW -5-(4-methylthiazanyl) —CH₃ —CH₃ CLX-5-(4-methylthiazanyl) —H —H CLY -5-(4-methylthiazanyl) —H —Cl CLZ-5-(4-methylthiazanyl) —H —Br CMA -5-(4-methylthiazanyl) —H —F CMB-5-(4-methylthiazanyl) —H —CH₃ CMC -5-(4-methylthiazanyl) —H —CF₃ CMD-5-(4-methylthiazanyl) —H —OCH₃ CME -5-(4-methylthiazanyl) —H —CH₂CH₃CMF -5-(4-methylthiazanyl) —H —OCF₃ CMG -5-(4-methylthiazanyl) —H-tert-butyl CMH -5-(4-methylthiazanyl) —H -iso-propyl

TABLE VII

and pharmaceutically acceptable salts thereof, wherein: Compound Ar₁ R₈R₉ CMI -2-pyridazinyl —Cl —H (a, b, and c) CMJ -2-pyridazinyl —Br —H (a,b, and c) CMK -2-pyridazinyl —F —H (a, b, and c) CML -2-pyridazinyl —CH₃—H (a, b, and c) CMM -2-pyridazinyl —CF₃ —H (a, b, and c) CMN-2-pyridazinyl —OCH₃ —H (a, b, and c) CMO -2-pyridazinyl —OCH₂CH₃ —H (a,b, and c) CMP -2-pyridazinyl —OCF₃ —H (a, b, and c) CMQ -2-pyridazinyl-tert-butyl —H (a, b, and c) CMR -2-pyridazinyl -iso-propyl —H (a, b,and c) CMS -2-pyridazinyl —CH₃ —CH₃ (a, b, and c) CMT -2-pyridazinyl —H—H (a, b, and c) CMU -2-pyridazinyl —H —Cl (a, b, and c) CMV-2-pyridazinyl —H —Br (a, b, and c) CMW -2-pyridazinyl —H —F (a, b, andc) CMX -2-pyridazinyl —H —CH₃ (a, b, and c) CMY -2-pyridazinyl —H —CF₃(a, b, and c) CMZ -2-pyridazinyl —H —OCH₃ (a, b, and c) CNA-2-pyridazinyl —H —OCH₂CH₃ (a, b, and c) CNB -2-pyridazinyl —H —OCF₃ (a,b, and c) CNC -2-pyridazinyl —H -tert-butyl (a, b, and c) CND-2-pyridazinyl —H -iso-propyl (a, b, and c) CNE -3-(4-chloropyridazinyl)—Cl —H (a, b, and c) CNF -3-(4-chloropyridazinyl) —Br —H (a, b, and c)CNG -3-(4-chloropyridazinyl) —F —H (a, b, and c) CNH-3-(4-chloropyridazinyl) —CH₃ —H (a, b, and c) CNI-3-(4-chloropyridazinyl) —CF₃ —H (a, b, and c) CNJ-3-(4-chloropyridazinyl) —OCH₃ —H (a, b, and c) CNK-3-(4-chloropyridazinyl) —OCH₂CH₃ —H (a, b, and c) CNL-3-(4-chloropyridazinyl) —OCF₃ —H (a, b, and c) CNM-3-(4-chloropyridazinyl) -tert-butyl —H (a, b, and c) CNN-3-(4-chloropyridazinyl) -iso-propyl —H (a, b, and c) CNO-3-(4-chloropyridazinyl) —CH₃ —CH₃ (a, b, and c) CNP-3-(4-chloropyridazinyl) —H —H (a, b, and c) CNQ-3-(4-chloropyridazinyl) —H —Cl (a, b, and c) CNR-3-(4-chloropyridazinyl) —H —Br (a, b, and c) CNS-3-(4-chloropyridazinyl) —H —F (a, b, and c) CNT-3-(4-chloropyridazinyl) —H —CH₃ (a, b, and c) CNU-3-(4-chloropyridazinyl) —H —CF₃ (a, b, and c) CNV-3-(4-chloropyridazinyl) —H —OCH₃ (a, b, and c) CNW-3-(4-chloropyridazinyl) —H —OCH₂CH₃ (a, b, and c) CNX-3-(4-chloropyridazinyl) —H —OCF₃ (a, b, and c) CNY-3-(4-chloropyridazinyl) —H -tert-butyl (a, b, and c) CNZ-3-(4-chloropyridazinyl) —H -iso-propyl (a, b, and c) COA-3-(4-methylpyridazinyl) —Cl —H (a, b, and c) COB-3-(4-methylpyridazinyl) —Br —H (a, b, and c) COC-3-(4-methylpyridazinyl) —F —H (a, b, and c) COD-3-(4-methylpyridazinyl) —CH₃ —H (a, b, and c) COE-3-(4-methylpyridazinyl) —CF₃ —H (a, b, and c) COF-3-(4-methylpyridazinyl) —OCH₃ —H (a, b, and c) COG-3-(4-methylpyridazinyl) —OCH₂CH₃ —H (a, b, and c) COH-3-(4-methylpyridazinyl) —OCF₃ —H (a, b, and c) COI-3-(4-methylpyridazinyl) -tert-butyl —H (a, b, and c) COJ-3-(4-methylpyridazinyl) -iso-propyl —H (a, b, and c) COK-3-(4-methylpyridazinyl) —CH₃ —CH₃ (a, b, and c) COL-3-(4-methylpyridazinyl) —H —H (a, b, and c) COM-3-(4-methylpyridazinyl) —H —Cl (a, b, and c) CON-3-(4-methylpyridazinyl) —H —Br (a, b, and c) COO-3-(4-methylpyridazinyl) —H —F (a, b, and c) COP-3-(4-methylpyridazinyl) —H —CH₃ (a, b, and c) COQ-3-(4-methylpyridazinyl) —H —CF₃ (a, b, and c) COR-3-(4-methylpyridazinyl) —H —OCH₃ (a, b, and c) COS-3-(4-methylpyridazinyl) —H —OCH₂CH₃ (a, b, and c) COT-3-(4-methylpyridazinyl) —H —OCF₃ (a, b, and c) COU-3-(4-methylpyridazinyl) —H -tert-butyl (a, b, and c) COV-3-(4-methylpyridazinyl) —H -iso-propyl (a, b, and c) COW -4-thiazanyl—Cl —H (a, b, and c) COX -4-thiazanyl —Br —H (a, b, and c) COY-4-thiazanyl —F —H (a, b, and c) COZ -4-thiazanyl —CH₃ —H (a, b, and c)CPA -4-thiazanyl —CF₃ —H (a, b, and c) CPB -4-thiazanyl —OCH₃ —H (a, b,and c) CPC -4-thiazanyl —OCH₂CH₃ —H (a, b, and c) CPD -4-thiazanyl —OCF₃—H (a, b, and c) CPE -4-thiazanyl -tert-butyl —H (a, b, and c) CPF-4-thiazanyl -iso-propyl —H (a, b, and c) CPG -4-thiazanyl —CH₃ —CH₃ (a,b, and c) CPH -4-thiazanyl —H —H (a, b, and c) CPI -4-thiazanyl —H —Cl(a, b, and c) CPJ -4-thiazanyl —H —Br (a, b, and c) CPK -4-thiazanyl —H—F (a, b, and c) CPL -4-thiazanyl —H —CH₃ (a, b, and c) CPM -4-thiazanyl—H —CF₃ (a, b, and c) CPN -4-thiazanyl —H —OCH₃ (a, b, and c) CPO-4-thiazanyl —H —OCH₂CH₃ (a, b, and c) CPP -4-thiazanyl —H —OCF₃ (a, b,and c) CPQ -4-thiazanyl —H -tert-butyl (a, b, and c) CPR -4-thiazanyl —H-iso-propyl (a, b, and c) CPS -5-(4-chlorothiazanyl) —Cl —H (a, b, andc) CPT -5-(4-chlorothiazanyl) —Br —H (a, b, and c) CPU-5-(4-chlorothiazanyl) —F —H (a, b, and c) CPV -5-(4-chlorothiazanyl)—CH₃ —H (a, b, and c) CPW -5-(4-chlorothiazanyl) —CF₃ —H (a, b, and c)CPX -5-(4-chlorothiazanyl) —OCH₃ —H (a, b, and c) CPY-5-(4-chlorothiazanyl) —OCH₂CH₃ —H (a, b, and c) CPZ-5-(4-chlorothiazanyl) —OCF₃ —H (a, b, and c) CQA -5-(4-chlorothiazanyl)-tert-butyl —H (a, b, and c) CQB -5-(4-chlorothiazanyl) -iso-propyl —H(a, b, and c) CQC -5-(4-chlorothiazanyl) —CH₃ —CH₃ (a, b, and c) CQD-5-(4-chlorothiazanyl) —H —H (a, b, and c) CQE -5-(4-chlorothiazanyl) —H—Cl (a, b, and c) CQF -5-(4-chlorothiazanyl) —H —Br (a, b, and c) CQG-5-(4-chlorothiazanyl) —H —F (a, b, and c) CQH -5-(4-chlorothiazanyl) —H—CH₃ (a, b, and c) CQI -5-(4-chlorothiazanyl) —H —CF₃ (a, b, and c) CQJ-5-(4-chlorothiazanyl) —H —OCH₃ (a, b, and c) CQK -5-(4-chlorothiazanyl)—H —OCH₂CH₃ (a, b, and c) CQL -5-(4-chlorothiazanyl) —H —OCF₃ (a, b, andc) CQM -5-(4-chlorothiazanyl) —H -tert-butyl (a, b, and c) CQN-5-(4-chlorothiazanyl) —H -iso-propyl (a, b, and c) CQO-5-(4-methylthiazanyl) —Cl —H (a, b, and c) CQP -5-(4-methylthiazanyl)—Br —H (a, b, and c) CQQ -5-(4-methylthiazanyl) —F —H (a, b, and c) CQR-5-(4-methylthiazanyl) —CH₃ —H (a, b, and c) CQS -5-(4-methylthiazanyl)—CF₃ —H (a, b, and c) CQT -5-(4-methylthiazanyl) —OCH₃ —H (a, b, and c)CQU -5-(4-methylthiazanyl) —OCH₂CH₃ —H (a, b, and c) CQV-5-(4-methylthiazanyl) —OCF₃ —H (a, b, and c) CQW -5-(4-methylthiazanyl)-tert-butyl —H (a, b, and c) CQX -5-(4-methylthiazanyl) -iso-propyl —H(a, b, and c) CQY -5-(4-methylthiazanyl) —CH₃ —CH₃ (a, b, and c) CQZ-5-(4-methylthiazanyl) —H —H (a, b, and c) CRA -5-(4-methylthiazanyl) —H—Cl (a, b, and c) CRB -5-(4-methylthiazanyl) —H —Br (a, b, and c) CRC-5-(4-methylthiazanyl) —H —F (a, b, and c) CRD -5-(4-methylthiazanyl) —H—CH₃ (a, b, and c) CRE -5-(4-methylthiazanyl) —H —CF₃ (a, b, and c) CRF-5-(4-methylthiazanyl) —H —OCH₃ (a, b, and c) CRG -5-(4-methylthiazanyl)—H —OCH₂CH₃ (a, b, and c) CRH -5-(4-methylthiazanyl) —H —OCF₃ (a, b, andc) CRI -5-(4-methylthiazanyl) —H -tert-butyl (a, b, and c) CRJ-5-(4-methylthiazanyl) —H -iso-propyl (a, b, and c) “a” means theBenzoazolylpiperazine Compound is racemic. “b” means the carbon atom ofthe piperazine ring attached to the methyl group is in the Rconfiguration. “c” means the carbon atom of the piperazine ring attachedto the methyl group is in the S configuration.

TABLE VIII

and pharmaceutically acceptable salts thereof, wherein: Compound Ar₁ R₈R₉ CRK -2-(3-chloropyridyl) —Cl —H (a, b, and c) CRL-2-(3-chloropyridyl) —Br —H (a, b, and c) CRM -2-(3-chloropyridyl) —F —H(a, b, and c) CRN -2-(3-chloropyridyl) —CH₃ —H (a, b, and c) CRO-2-(3-chloropyridyl) —CF₃ —H (a, b, and c) CRP -2-(3-chloropyridyl)—OCH₃ —H (a, b, and c) CRQ -2-(3-chloropyridyl) —OCH₂CH₃ —H (a, b, andc) CRR -2-(3-chloropyridyl) —OCF₃ —H (a, b, and c) CRS-2-(3-chloropyridyl) -tert-butyl —H (a, b, and c) CRT-2-(3-chloropyridyl) -iso-propyl —H (a, b, and c) CRU-2-(3-chloropyridyl) —CH₃ —CH₃ (a, b, and c) CRV -2-(3-chloropyridyl) —H—H (a, b, and c) CRW -2-(3-chloropyridyl) —H —Cl (a, b, and c) CRX-2-(3-chloropyridyl) —H —Br (a, b, and c) CRY -2-(3-chloropyridyl) —H —F(a, b, and c) CRZ -2-(3-chloropyridyl) —H —CH₃ (a, b, and c) CSA-2-(3-chloropyridyl) —H —CF₃ (a, b, and c) CSB -2-(3-chloropyridyl) —H—OCH₃ (a, b, and c) CSC -2-(3-chloropyridyl) —H —OCH₂CH₃ (a, b, and c)CSD -2-(3-chloropyridyl) —H —OCF₃ (a, b, and c) CSE -2-(3-chloropyridyl)—H -tert-butyl (a, b, and c) CSF -2-(3-chloropyridyl) —H -iso-propyl (a,b, and c) CSG -2-(3-methylpyridyl) —Cl —H (a, b, and c) CSH-2-(3-methylpyridyl) —Br —H (a, b, and c) CSI -2-(3-methylpyridyl) —F —H(a, b, and c) CSJ -2-(3-methylpyridyl) —CH₃ —H (a, b, and c) CSK-2-(3-methylpyridyl) —CF₃ —H (a, b, and c) CSL -2-(3-methylpyridyl)—OCH₃ —H (a, b, and c) CSM -2-(3-methylpyridyl) —OCH₂CH₃ —H (a, b, andc) CSN -2-(3-methylpyridyl) —OCF₃ —H (a, b, and c) CSO-2-(3-methylpyridyl) -tert-butyl —H (a, b, and c) CSP-2-(3-methylpyridyl) -iso-propyl —H (a, b, and c) CSQ-2-(3-methylpyridyl) —CH₃ —CH₃ (a, b, and c) CSR -2-(3-methylpyridyl) —H—H (a, b, and c) CSS -2-(3-methylpyridyl) —H —Cl (a, b, and c) CST-2-(3-methylpyridyl) —H —Br (a, b, and c) CSU -2-(3-methylpyridyl) —H —F(a, b, and c) CSV -2-(3-methylpyridyl) —H —CH₃ (a, b, and c) CSW-2-(3-methylpyridyl) —H —CF₃ (a, b, and c) CSX -2-(3-methylpyridyl) —H—OCH₃ (a, b, and c) CSY -2-(3-methylpyridyl) —H —OCH₂CH₃ (a, b, and c)CSZ -2-(3-methylpyridyl) —H —OCF₃ (a, b, and c) CTA -2-(3-methylpyridyl)—H -tert-butyl (a, b, and c) CTB -2-(3-methylpyridyl) —H -iso-propyl (a,b, and c) CTC -2-(3-CF₃-pyridyl) —Cl —H (a, b, and c) CTD-2-(3-CF₃-pyridyl) —Br —H (a, b, and c) CTE -2-(3-CF₃-pyridyl) —F —H (a,b, and c) CTF -2-(3-CF₃-pyridyl) —CH₃ —H (a, b, and c) CTG-2-(3-CF₃-pyridyl) —CF₃ —H (a, b, and c) CTH -2-(3-CF₃-pyridyl) —OCH₃ —H(a, b, and c) CTI -2-(3-CF₃-pyridyl) —OCH₂CH₃ —H (a, b, and c) CTJ-2-(3-CF₃-pyridyl) —OCF₃ —H (a, b, and c) CTK -2-(3-CF₃-pyridyl)-tert-butyl —H (a, b, and c) CTL -2-(3-CF₃-pyridyl) -iso-propyl —H (a,b, and c) CTM -2-(3-CF₃-pyridyl) —CH₃ —CH₃ (a, b, and c) CTN-2-(3-CF₃-pyridyl) —H —H (a, b, and c) CTO -2-(3-CF₃-pyridyl) —H —Cl (a,b, and c) CTP -2-(3-CF₃-pyridyl) —H —Br (a, b, and c) CTQ-2-(3-CF₃-pyridyl) —H —F (a, b, and c) CTR -2-(3-CF₃-pyridyl) —H —CH₃(a, b, and c) CTS -2-(3-CF₃-pyridyl) —H —CF₃ (a, b, and c) CTT-2-(3-CF₃-pyridyl) —H —OCH₃ (a, b, and c) CTU -2-(3-CF₃-pyridyl) —H—OCH₂CH₃ (a, b, and c) CTV -2-(3-CF₃-pyridyl) —H —OCF₃ (a, b, and c) CTW-2-(3-CF₃-pyridyl) —H -tert-butyl (a, b, and c) CTX -2-(3-CF₃-pyridyl)—H -iso-propyl (a, b, and c) CTY -4-(5-chloropyrimidinyl) —Cl —H (a, b,and c) CTZ -4-(5-chloropyrimidinyl) —Br —H (a, b, and c) CUA-4-(5-chloropyrimidinyl) —F —H (a, b, and c) CUB-4-(5-chloropyrimidinyl) —CH₃ —H (a, b, and c) CUC-4-(5-chloropyrimidinyl) —CF₃ —H (a, b, and c) CUD-4-(5-chloropyrimidinyl) —OCH₃ —H (a, b, and c) CUE-4-(5-chloropyrimidinyl) —OCH₂CH₃ —H (a, b, and c) CUF-4-(5-chloropyrimidinyl) —OCF₃ —H (a, b, and c) CUG-4-(5-chloropyrimidinyl) -tert-butyl —H (a, b, and c) CUH-4-(5-chloropyrimidinyl) -iso-propyl —H (a, b, and c) CUI-4-(5-chloropyrimidinyl) —CH₃ —CH₃ (a, b, and c) CUJ-4-(5-chloropyrimidinyl) —H —H (a, b, and c) CUK-4-(5-chloropyrimidinyl) —H —Cl (a, b, and c) CUL-4-(5-chloropyrimidinyl) —H —Br (a, b, and c) CUM-4-(5-chloropyrimidinyl) —H —F (a, b, and c) CUN-4-(5-chloropyrimidinyl) —H —CH₃ (a, b, and c) CUO-4-(5-chloropyrimidinyl) —H —CF₃ (a, b, and c) CUP-4-(5-chloropyrimidinyl) —H —OCH₃ (a, b, and c) CUQ-4-(5-chloropyrimidinyl) —H —OCH₂CH₃ (a, b, and c) CUR-4-(5-chloropyrimidinyl) —H —OCF₃ (a, b, and c) CUS-4-(5-chloropyrimidinyl) —H -tert-butyl (a, b, and c) CUT-4-(5-chloropyrimidinyl) —H -iso-propyl (a, b, and c) CUU-4-(5-methylpyrimidinyl) —Cl —H (a, b, and c) CUV-4-(5-methylpyrimidinyl) —Br —H (a, b, and c) CUW-4-(5-methylpyrimidinyl) —F —H (a, b, and c) CUX-4-(5-methylpyrimidinyl) —CH₃ —H (a, b, and c) CUY-4-(5-methylpyrimidinyl) —CF₃ —H (a, b, and c) CUZ-4-(5-methylpyrimidinyl) —OCH₃ —H (a, b, and c) CVA-4-(5-methylpyrimidinyl) —OCH₂CH₃ —H (a, b, and c) CVB-4-(5-methylpyrimidinyl) —OCF₃ —H (a, b, and c) CVC-4-(5-methylpyrimidinyl) -tert-butyl —H (a, b, and c) CVD-4-(5-methylpyrimidinyl) -iso-propyl —H (a, b, and c) CVE-4-(5-methylpyrimidinyl) —CH₃ —CH₃ (a, b, and c) CVF-4-(5-methylpyrimidinyl) —H —H (a, b, and c) CVG-4-(5-methylpyrimidinyl) —H —Cl (a, b, and c) CVH-4-(5-methylpyrimidinyl) —H —Br (a, b, and c) CVI-4-(5-methylpyrimidinyl) —H —F (a, b, and c) CVJ-4-(5-methylpyrimidinyl) —H —CH₃ (a, b, and c) CVK-4-(5-methylpyrimidinyl) —H —CF₃ (a, b, and c) CVL-4-(5-methylpyrimidinyl) —H —OCH₃ (a, b, and c) CVM-4-(5-methylpyrimidinyl) —H —OCH₂CH₃ (a, b, and c) CVN-4-(5-methylpyrimidinyl) —H —OCF₃ (a, b, and c) CVO-4-(5-methylpyrimidinyl) —H -tert-butyl (a, b, and c) CVP-4-(5-methylpyrimidinyl) —H -iso-propyl (a, b, and c) CVQ -2-pyrazinyl—Cl —H (a, b, and c) CVR -2-pyrazinyl —Br —H (a, b, and c) CVS-2-pyrazinyl —F —H (a, b, and c) CVT -2-pyrazinyl —CH₃ —H (a, b, and c)CVU -2-pyrazinyl —CF₃ —H (a, b, and c) CVV -2-pyrazinyl —OCH₃ —H (a, b,and c) CVW -2-pyrazinyl —OCH₂CH₃ —H (a, b, and c) CVX -2-pyrazinyl —OCF₃—H (a, b, and c) CVY -2-pyrazinyl -tert-butyl —H (a, b, and c) CVZ-2-pyrazinyl -iso-propyl —H (a, b, and c) CWA -2-pyrazinyl —CH₃ —CH₃ (a,b, and c) CWB -2-pyrazinyl —H —H (a, b, and c) CWC -2-pyrazinyl —H —Cl(a, b, and c) CWD -2-pyrazinyl —H —Br (a, b, and c) CWE -2-pyrazinyl —H—F (a, b, and c) CWF -2-pyrazinyl —H —CH₃ (a, b, and c) CWG -2-pyrazinyl—H —CF₃ (a, b, and c) CWH -2-pyrazinyl —H —OCH₃ (a, b, and c) CWI-2-pyrazinyl —H —OCH₂CH₃ (a, b, and c) CWJ -2-pyrazinyl —H —OCF₃ (a, b,and c) CWK -2-pyrazinyl —H -tert-butyl (a, b, and c) CWL -2-pyrazinyl —H-iso-propyl (a, b, and c) CWM -2-(3-chloropyrazinyl) —Cl —H (a, b, andc) CWN -2-(3-chloropyrazinyl) —Br —H (a, b, and c) CWO-2-(3-chloropyrazinyl) —F —H (a, b, and c) CWP -2-(3-chloropyrazinyl)—CH₃ —H (a, b, and c) CWQ -2-(3-chloropyrazinyl) —CF₃ —H (a, b, and c)CWR -2-(3-chloropyrazinyl) —OCH₃ —H (a, b, and c) CWS-2-(3-chloropyrazinyl) —OCH₂CH₃ —H (a, b, and c) CWT-2-(3-chloropyrazinyl) —OCF₃ —H (a, b, and c) CWU -2-(3-chloropyrazinyl)-tert-butyl —H (a, b, and c) CWV -2-(3-chloropyrazinyl) -iso-propyl —H(a, b, and c) CWW -2-(3-chloropyrazinyl) —CH₃ —CH₃ (a, b, and c) CWX-2-(3-chloropyrazinyl) —H —H (a, b, and c) CWY -2-(3-chloropyrazinyl) —H—Cl (a, b, and c) CWZ -2-(3-chloropyrazinyl) —H —Br (a, b, and c) CXA-2-(3-chloropyrazinyl) —H —F (a, b, and c) CXB -2-(3-chloropyrazinyl) —H—CH₃ (a, b, and c) CXC -2-(3-chloropyrazinyl) —H —CF₃ (a, b, and c) CXD-2-(3-chloropyrazinyl) —H —OCH₃ (a, b, and c) CXE -2-(3-chloropyrazinyl)—H —OCH₂CH₃ (a, b, and c) CXF -2-(3-chloropyrazinyl) —H —OCF₃ (a, b, andc) CXG -2-(3-chloropyrazinyl) —H -tert-butyl (a, b, and c) CXH-2-(3-chloropyrazinyl) —H -iso-propyl (a, b, and c) CXI-2-(3-methylpyrazinyl) —Cl —H (a, b, and c) CXJ -2-(3-methylpyrazinyl)—Br —H (a, b, and c) CXK -2-(3-methylpyrazinyl) —F —H (a, b, and c) CXL-2-(3-methylpyrazinyl) —CH₃ —H (a, b, and c) CXM -2-(3-methylpyrazinyl)—CF₃ —H (a, b, and c) CXN -2-(3-methylpyrazinyl) —OCH₃ —H (a, b, and c)CXO -2-(3-methylpyrazinyl) —OCH₂CH₃ —H (a, b, and c) CXP-2-(3-methylpyrazinyl) —OCF₃ —H (a, b, and c) CXQ -2-(3-methylpyrazinyl)-tert-butyl —H (a, b, and c) CXR -2-(3-methylpyrazinyl) -iso-propyl —H(a, b, and c) CXS -2-(3-methylpyrazinyl) —CH₃ —CH₃ (a, b, and c) CXT-2-(3-methylpyrazinyl) —H —H (a, b, and c) CXU -2-(3-methylpyrazinyl) —H—Cl (a, b, and c) CXV -2-(3-methylpyrazinyl) —H —Br (a, b, and c) CXW-2-(3-methylpyrazinyl) —H —F (a, b, and c) CXX -2-(3-methylpyrazinyl) —H—CH₃ (a, b, and c) CXY -2-(3-methylpyrazinyl) —H —CF₃ (a, b, and c) CXZ-2-(3-methylpyrazinyl) —H —OCH₃ (a, b, and c) CYA -2-(3-methylpyrazinyl)—H —OCH₂CH₃ (a, b, and c) CYB -2-(3-methylpyrazinyl) —H —OCF₃ (a, b, andc) CYC -2-(3-methylpyrazinyl) —H -tert-butyl (a, b, and c) CYD-2-(3-methylpyrazinyl) —H -iso-propyl (a, b, and c) CYE -2-pyridazinyl—Cl —H (a, b, and c) CYF -2-pyridazinyl —Br —H (a, b, and c) CYG-2-pyridazinyl —F —H (a, b, and c) CYH -2-pyridazinyl —CH₃ —H (a, b, andc) CYI -2-pyridazinyl —CF₃ —H (a, b, and c) CYJ -2-pyridazinyl —OCH₃ —H(a, b, and c) CYK -2-pyridazinyl —OCH₂CH₃ —H (a, b, and c) CYL-2-pyridazinyl —OCF₃ —H (a, b, and c) CYM -2-pyridazinyl -tert-butyl —H(a, b, and c) CYN -2-pyridazinyl -iso-propyl —H (a, b, and c) CYO-2-pyridazinyl —CH₃ —CH₃ (a, b, and c) CYP -2-pyridazinyl —H —H (a, b,and c) CYQ -2-pyridazinyl —H —Cl (a, b, and c) CYR -2-pyridazinyl —H —Br(a, b, and c) CYS -2-pyridazinyl —H —F (a, b, and c) CYT -2-pyridazinyl—H —CH₃ (a, b, and c) CYU -2-pyridazinyl —H —CF₃ (a, b, and c) CYV-2-pyridazinyl —H —OCH₃ (a, b, and c) CYW -2-pyridazinyl —H —OCH₂CH₂ (a,b, and c) CYX -2-pyridazinyl —H —OCF₃ (a, b, and c) CYY -2-pyridazinyl—H -tert-butyl (a, b, and c) CYZ -2-pyridazinyl —H -iso-propyl (a, b,and c) CZA -3-(4-chloropyridazinyl) —Cl —H (a, b, and c) CZB-3-(4-chloropyridazinyl) —Br —H (a, b, and c) CZC-3-(4-chloropyridazinyl) —F —H (a, b, and c) CZD-3-(4-chloropyridazinyl) —CH₃ —H (a, b, and c) CZE-3-(4-chloropyridazinyl) —CF₃ —H (a, b, and c) CZF-3-(4-chloropyridazinyl) —OCH₃ —H (a, b, and c) CZG-3-(4-chloropyridazinyl) —OCH₂CH₃ —H (a, b, and c) CZH-3-(4-chloropyridazinyl) —OCF₃ —H (a, b, and c) CZI-3-(4-chloropyridazinyl) -tert-butyl —H (a, b, and c) CZJ-3-(4-chloropyridazinyl) -iso-propyl —H (a, b, and c) CZK-3-(4-chloropyridazinyl) —CH₃ —CH₃ (a, b, and c) CZL-3-(4-chloropyridazinyl) —H —H (a, b, and c) CZM-3-(4-chloropyridazinyl) —H —Cl (a, b, and c) CZN-3-(4-chloropyridazinyl) —H —Br (a, b, and c) CZO-3-(4-chloropyridazinyl) —H —F (a, b, and c) CZP-3-(4-chloropyridazinyl) —H —CH₃ (a, b, and c) CZQ-3-(4-chloropyridazinyl) —H —CF₃ (a, b, and c) CZR-3-(4-chloropyridazinyl) —H —OCH₃ (a, b, and c) CZS-3-(4-chloropyridazinyl) —H —OCH₂CH₂ (a, b, and c) CZT-3-(4-chloropyridazinyl) —H —OCF₃ (a, b, and c) CZU-3-(4-chloropyridazinyl) —H -tert-butyl (a, b, and c) CZV-3-(4-chloropyridazinyl) —H -iso-propyl (a, b, and c) CZW-3-(4-methylpyridazinyl) —Cl —H (a, b, and c) CZX-3-(4-methylpyridazinyl) —Br —H (a, b, and c) CZY-3-(4-methylpyridazinyl) —F —H (a, b, and c) CZZ-3-(4-methylpyridazinyl) —CH₃ —H (a, b, and c) DAA-3-(4-methylpyridazinyl) —CF₃ —H (a, b, and c) DAB-3-(4-methylpyridazinyl) —OCH₃ —H (a, b, and c) DAC-3-(4-methylpyridazinyl) —OCH₂CH₃ —H (a, b, and c) DAD-3-(4-methylpyridazinyl) —OCF₃ —H (a, b, and c) DAE-3-(4-methylpyridazinyl) -tert-butyl —H (a, b, and c) DAF-3-(4-methylpyridazinyl) -iso-propyl —H (a, b, and c) DAG-3-(4-methylpyridazinyl) —CH₃ —CH₃ (a, b, and c) DAH-3-(4-methylpyridazinyl) —H —H (a, b, and c) DAI-3-(4-methylpyridazinyl) —H —Cl (a, b, and c) DAJ-3-(4-methylpyridazinyl) —H —Br (a, b, and c) DAK-3-(4-methylpyridazinyl) —H —F (a, b, and c) DAL-3-(4-methylpyridazinyl) —H —CH₃ (a, b, and c) DAM-3-(4-methylpyridazinyl) —H —CF₃ (a, b, and c) DAN-3-(4-methylpyridazinyl) —H —OCH₃ (a, b, and c) DAO-3-(4-methylpyridazinyl) —H —OCH₂CH₃ (a, b, and c) DAP-3-(4-methylpyridazinyl) —H —OCF₃ (a, b, and c) DAQ-3-(4-methylpyridazinyl) —H -tert-butyl (a, b, and c) DAR-3-(4-methylpyridazinyl) —H -iso-propyl (a, b, and c) DAS -4-thiazanyl—Cl —H (a, b, and c) DAT -4-thiazanyl —Br —H (a, b, and c) DAU-4-thiazanyl —F —H (a, b, and c) DAV -4-thiazanyl —CH₃ —H (a, b, and c)DAW -4-thiazanyl —CF₃ —H (a, b, and c) DAX -4-thiazanyl —OCH₃ —H (a, b,and c) DAY -4-thiazanyl —OCH₂CH₃ —H (a, b, and c) DAZ -4-thiazanyl —OCF₃—H (a, b, and c) DBA -4-thiazanyl -tert-butyl —H (a, b, and c) DBB-4-thiazanyl -iso-propyl —H (a, b, and c) DBC -4-thiazanyl —CH₃ —CH₃ (a,b, and c) DBD -4-thiazanyl —H —H (a, b, and c) DBE -4-thiazanyl —H —Cl(a, b, and c) DBF -4-thiazanyl —H —Br (a, b, and c) DBG -4-thiazanyl —H—F (a, b, and c) DBH -4-thiazanyl —H —CH₃ (a, b, and c) DBI -4-thiazanyl—H —CF₃ (a, b, and c) DBJ -4-thiazanyl —H —OCH₃ (a, b, and c) DBK-4-thiazanyl —H —OCH₂CH₃ (a, b, and c) DBL -4-thiazanyl —H —OCF₃ (a, b,and c) DBM -4-thiazanyl —H -tert-butyl (a, b, and c) DBN -4-thiazanyl —H-iso-propyl (a, b, and c) DBO -5-(4-chlorothiazanyl) —Cl —H (a, b, andc) DBP -5-(4-chlorothiazanyl) —Br —H (a, b, and c) DBQ-5-(4-chlorothiazanyl) —F —H (a, b, and c) DBR -5-(4-chlorothiazanyl)—CH₃ —H (a, b, and c) DBS -5-(4-chlorothiazanyl) —CF₃ —H (a, b, and c)DBT -5-(4-chlorothiazanyl) —OCH₃ —H (a, b, and c) DBU-5-(4-chlorothiazanyl) —OCH₂CH₃ —H (a, b, and c) DBV-5-(4-chlorothiazanyl) —OCF₃ —H (a, b, and c) DBW -5-(4-chlorothiazanyl)-tert-butyl —H (a, b, and c) DBX -5-(4-chlorothiazanyl) -iso-propyl —H(a, b, and c) DBY -5-(4-chlorothiazanyl) —CH₃ —CH₃ (a, b, and c) DBZ-5-(4-chlorothiazanyl) —H —H (a, b, and c) DCA -5-(4-chlorothiazanyl) —H—Cl (a, b, and c) DCB -5-(4-chlorothiazanyl) —H —Br (a, b, and c) DCC-5-(4-chlorothiazanyl) —H —F (a, b, and c) DCD -5-(4-chlorothiazanyl) —H—CH₃ (a, b, and c) DCE -5-(4-chlorothiazanyl) —H —CF₃ (a, b, and c) DCF-5-(4-chlorothiazanyl) —H —OCH₃ (a, b, and c) DCG -5-(4-chlorothiazanyl)—H —OCH₂CH₃ (a, b, and c) DCH -5-(4-chlorothiazanyl) —H —OCF₃ (a, b, andc) DCI -5-(4-chlorothiazanyl) —H -tert-butyl (a, b, and c) DCJ-5-(4-chlorothiazanyl) —H -iso-propyl (a, b, and c) DCK-5-(4-methylthiazanyl) —Cl —H (a, b, and c) DCL -5-(4-methylthiazanyl)—Br —H (a, b, and c) DCM -5-(4-methylthiazanyl) —F —H (a, b, and c) DCN-5-(4-methylthiazanyl) —CH₃ —H (a, b, and c) DCO -5-(4-methylthiazanyl)—CF₃ —H (a, b, and c) DCP -5-(4-methylthiazanyl) —OCH₃ —H (a, b, and c)DCQ -5-(4-methylthiazanyl) —OCH₂CH₃ —H (a, b, and c) DCR-5-(4-methylthiazanyl) —OCF₃ —H (a, b, and c) DCS -5-(4-methylthiazanyl)-tert-butyl —H (a, b, and c) DCT -5-(4-methylthiazanyl) -iso-propyl —H(a, b, and c) DCU -5-(4-methylthiazanyl) —CH₃ —CH₃ (a, b, and c) DCV-5-(4-methylthiazanyl) —H —H (a, b, and c) DCW -5-(4-methylthiazanyl) —H—Cl (a, b, and c) DCX -5-(4-methylthiazanyl) —H —Br (a, b, and c) DCY-5-(4-methylthiazanyl) —H —F (a, b, and c) DCZ -5-(4-methylthiazanyl) —H—CH₃ (a, b, and c) DDA -5-(4-methylthiazanyl) —H —CF₃ (a, b, and c) DDB-5-(4-methylthiazanyl) —H —OCH₃ (a, b, and c) DDC -5-(4-methylthiazanyl)—H —OCH₂CH₃ (a, b, and c) DDD -5-(4-methylthiazanyl) —H —OCF₃ (a, b, andc) DDE -5-(4-methylthiazanyl) —H -tert-butyl (a, b, and c) DDF-5-(4-methylthiazanyl) —H -iso-propyl “a” means theBenzoazolylpiperazine Compound is racemic. “b” means the carbon atom ofthe piperazine ring attached to the methyl group is in the Rconfiguration. “c” means the carbon atom of the piperazine ring attachedto the methyl group is in the S configuration.

TABLE IX

and pharmaceutically acceptable salts thereof, wherein: Compound Ar₁ R₈R₉ DDG -2-pyridazinyl —Cl —H DDH -2-pyridazinyl —Br —H DDI-2-pyridazinyl —F —H DDJ -2-pyridazinyl —CH₃ —H DDK -2-pyridazinyl —CF₃—H DDL -2-pyridazinyl —OCH₃ —H DDM -2-pyridazinyl —OCH₂CH₃ —H DDN-2-pyridazinyl —OCF₃ —H DDO -2-pyridazinyl -tert-butyl —H DDP-2-pyridazinyl -iso-propyl —H DDQ -2-pyridazinyl —CH₃ —CH₃ DDR-2-pyridazinyl —H —H DDS -2-pyridazinyl —H —Cl DDT -2-pyridazinyl —H —BrDDU -2-pyridazinyl —H —F DDV -2-pyridazinyl —H —CH₃ DDW -2-pyridazinyl—H —CF₃ DDX -2-pyridazinyl —H —OCH₃ DDY -2-pyridazinyl —H —OCH₂CH₃ DDZ-2-pyridazinyl —H —OCF₃ DEA -2-pyridazinyl —H -tert-butyl DEB-2-pyridazinyl —H -iso-propyl DEC -3-(4-chloropyridazinyl) —Cl —H DED-3-(4-chloropyridazinyl) —Br —H DEE -3-(4-chloropyridazinyl) —F —H DEF-3-(4-chloropyridazinyl) —CH₃ —H DEG -3-(4-chloropyridazinyl) —CF₃ —HDEH -3-(4-chloropyridazinyl) —OCH₃ —H DEI -3-(4-chloropyridazinyl)—OCH₂CH₃ —H DEJ -3-(4-chloropyridazinyl) —OCF₃ —H DEK-3-(4-chloropyridazinyl) -tert-butyl —H DEL -3-(4-chloropyridazinyl)-iso-propyl —H DEM -3-(4-chloropyridazinyl) —CH₃ —CH₃ DEN-3-(4-chloropyridazinyl) —H —H DEO -3-(4-chloropyridazinyl) —H —Cl DEP-3-(4-chloropyridazinyl) —H —Br DEQ -3-(4-chloropyridazinyl) —H —F DER-3-(4-chloropyridazinyl) —H —CH₃ DES -3-(4-chloropyridazinyl) —H —CF₃DET -3-(4-chloropyridazinyl) —H —OCH₃ DEU -3-(4-chloropyridazinyl) —H—OCH₂CH₃ DEV -3-(4-chloropyridazinyl) —H —OCF₃ DEW-3-(4-chloropyridazinyl) —H -tert-butyl DEX -3-(4-chloropyridazinyl) —H-iso-propyl DEY -3-(4-methylpyridazinyl) —Cl —H DEZ-3-(4-methylpyridazinyl) —Br —H DFA -3-(4-methylpyridazinyl) —F —H DFB-3-(4-methylpyridazinyl) —CH₃ —H DFC -3-(4-methylpyridazinyl) —CF₃ —HDFD -3-(4-methylpyridazinyl) —OCH₃ —H DFE -3-(4-methylpyridazinyl)—OCH₂CH₃ —H DFF -3-(4-methylpyridazinyl) —OCF₃ —H DFG-3-(4-methylpyridazinyl) -tert-butyl —H DFH -3-(4-methylpyridazinyl)-iso-propyl —H DFI -3-(4-methylpyridazinyl) —CH₃ —CH₃ DFJ-3-(4-methylpyridazinyl) —H —H DFK -3-(4-methylpyridazinyl) —H —Cl DFL-3-(4-methylpyridazinyl) —H —Br DFM -3-(4-methylpyridazinyl) —H —F DFN-3-(4-methylpyridazinyl) —H —CH₃ DFO -3-(4-methylpyridazinyl) —H —CF₃DFP -3-(4-methylpyridazinyl) —H —OCH₃ DFQ -3-(4-methylpyridazinyl) —H—OCH₂CH₃ DFR -3-(4-methylpyridazinyl) —H —OCF₃ DFS-3-(4-methylpyridazinyl) —H -tert-butyl DFT -3-(4-methylpyridazinyl) —H-iso-propyl DFU -4-thiazanyl —Cl —H DFV -4-thiazanyl —Br —H DFW-4-thiazanyl —F —H DFX -4-thiazanyl —CH₃ —H DFY -4-thiazanyl —CF₃ —H DFZ-4-thiazanyl —OCH₃ —H DGA -4-thiazanyl —OCH₂CH₃ —H DGB -4-thiazanyl—OCF₃ —H DGC -4-thiazanyl -tert-butyl —H DGD -4-thiazanyl -iso-propyl —HDGE -4-thiazanyl —CH₃ —CH₃ DGF -4-thiazanyl —H —H DGG -4-thiazanyl —H—Cl DGH -4-thiazanyl —H —Br DGI -4-thiazanyl —H —F DGJ -4-thiazanyl —H—CH₃ DGK -4-thiazanyl —H —CF₃ DGL -4-thiazanyl —H —OCH₃ DGM -4-thiazanyl—H —OCH₂CH₃ DGN -4-thiazanyl —H —OCF₃ DGO -4-thiazanyl —H -tert-butylDGP -4-thiazanyl —H -iso-propyl DGQ -5-(4-chlorothiazanyl) —Cl —H DGR-5-(4-chlorothiazanyl) —Br —H DGS -5-(4-chlorothiazanyl) —F —H DGT-5-(4-chlorothiazanyl) —CH₃ —H DGU -5-(4-chlorothiazanyl) —CF₃ —H DGV-5-(4-chlorothiazanyl) —OCH₃ —H DGW -5-(4-chlorothiazanyl) —OCH₂CH₃ —HDGX -5-(4-chlorothiazanyl) —OCF₃ —H DGY -5-(4-chlorothiazanyl)-tert-butyl —H DGZ -5-(4-chlorothiazanyl) -iso-propyl —H DHA-5-(4-chlorothiazanyl) —CH₃ —CH₃ DHB -5-(4-chlorothiazanyl) —H —H DHC-5-(4-chlorothiazanyl) —H —Cl DHD -5-(4-chlorothiazanyl) —H —Br DHE-5-(4-chlorothiazanyl) —H —F DHF -5-(4-chlorothiazanyl) —H —CH₃ DHG-5-(4-chlorothiazanyl) —H —CF₃ DHH -5-(4-chlorothiazanyl) —H —OCH₃ DHI-5-(4-chlorothiazanyl) —H —OCH₂CH₃ DHJ -5-(4-chlorothiazanyl) —H —OCF₃DHK -5-(4-chlorothiazanyl) —H -tert-butyl DHL -5-(4-chlorothiazanyl) —H-iso-propyl DHM -5-(4-methylthiazanyl) —Cl —H DHN -5-(4-methylthiazanyl)—Br —H DHO -5-(4-methylthiazanyl) —F —H DHP -5-(4-methylthiazanyl) —CH₃—H DHQ -5-(4-methylthiazanyl) —CF₃ —H DHR -5-(4-methylthiazanyl) —OCH₃—H DHS -5-(4-methylthiazanyl) —OCH₂CH₃ —H DHT -5-(4-methylthiazanyl)—OCF₃ —H DHU -5-(4-methylthiazanyl) -tert-butyl —H DHV-5-(4-methylthiazanyl) -iso-propyl —H DHW -5-(4-methylthiazanyl) —CH₃—CH₃ DHX -5-(4-methylthiazanyl) —H —H DHY -5-(4-methylthiazanyl) —H —ClDHZ -5-(4-methylthiazanyl) —H —Br DIA -5-(4-methylthiazanyl) —H —F DIB-5-(4-methylthiazanyl) —H —CH₃ DIC -5-(4-methylthiazanyl) —H —CF₃ DID-5-(4-methylthiazanyl) —H —OCH₃ DIE -5-(4-methylthiazanyl) —H —OCH₂CH₃DIF -5-(4-methylthiazanyl) —H —OCF₃ DIG -5-(4-methylthiazanyl) —H-tert-butyl DIH -5-(4-methylthiazanyl) —H -iso-propyl

TABLE X

and pharmaceutically acceptable salts thereof, wherein: Compound Ar₁ R₈R₉ DII -2-(3-chloropyridyl) —Cl —H DIJ -2-(3-chloropyridyl) —Br —H DIK-2-(3-chloropyridyl) —F —H DIL -2-(3-chloropyridyl) —CH₃ —H DIM-2-(3-chloropyridyl) —CF₃ —H DIN -2-(3-chloropyridyl) —OCH₃ —H DIO-2-(3-chloropyridyl) —OCH₂CH₃ —H DIP -2-(3-chloropyridyl) —OCF₃ —H DIQ-2-(3-chloropyridyl) -tert-butyl —H DIR -2-(3-chloropyridyl) -iso-propyl—H DIS -2-(3-chloropyridyl) —CH₃ —CH₃ DIT -2-(3-chloropyridyl) —H —H DIU-2-(3-chloropyridyl) —H —Cl DIV -2-(3-chloropyridyl) —H —Br DIW-2-(3-chloropyridyl) —H —F DIX -2-(3-chloropyridyl) —H —CH₃ DIY-2-(3-chloropyridyl) —H —CF₃ DIZ -2-(3-chloropyridyl) —H —OCH₃ DJA-2-(3-chloropyridyl) —H —OCH₂CH₃ DJB -2-(3-chloropyridyl) —H —OCF₃ DJC-2-(3-chloropyridyl) —H -tert-butyl DJD -2-(3-chloropyridyl) —H-iso-propyl DJE -2-(3-methylpyridyl) —Cl —H DJF -2-(3-methylpyridyl) —Br—H DJG -2-(3-methylpyridyl) —F —H DJH -2-(3-methylpyridyl) —CH₃ —H DJI-2-(3-methylpyridyl) —CF₃ —H DJJ -2-(3-methylpyridyl) —OCH₃ —H DJK-2-(3-methylpyridyl) —OCH₂CH₃ —H DJL -2-(3-methylpyridyl) —OCF₃ —H DJM-2-(3-methylpyridyl) -tert-butyl —H DJN -2-(3-methylpyridyl) -iso-propyl—H DJO -2-(3-methylpyridyl) —CH₃ —CH₃ DJP -2-(3-methylpyridyl) —H —H DJQ-2-(3-methylpyridyl) —H —Cl DJR -2-(3-methylpyridyl) —H —Br DJS-2-(3-methylpyridyl) —H —F DJT -2-(3-methylpyridyl) —H —CH₃ DJU-2-(3-methylpyridyl) —H —CF₃ DJV -2-(3-methylpyridyl) —H —OCH₃ DJW-2-(3-methylpyridyl) —H —OCH₂CH₃ DJX -2-(3-methylpyridyl) —H —OCF₃ DJY-2-(3-methylpyridyl) —H -tert-butyl DJZ -2-(3-methylpyridyl) —H-iso-propyl DKA -2-(3-CF₃-pyridyl) —Cl —H DKB -2-(3-CF₃-pyridyl) —Br —HDKC -2-(3-CF₃-pyridyl) —F —H DKD -2-(3-CF₃-pyridyl) —CH₃ —H DKE-2-(3-CF₃-pyridyl) —CF₃ —H DKF -2-(3-CF₃-pyridyl) —OCH₃ —H DKG-2-(3-CF₃-pyridyl) —OCH₂CH₃ —H DKH -2-(3-CF₃-pyridyl) —OCF₃ —H DKI-2-(3-CF₃-pyridyl) -tert-butyl —H DKJ -2-(3-CF₃-pyridyl) -iso-propyl —HDKK -2-(3-CF₃-pyridyl) —CH₃ —CH₃ DKL -2-(3-CF₃-pyridyl) —H —H DKM-2-(3-CF₃-pyridyl) —H —Cl DKN -2-(3-CF₃-pyridyl) —H —Br DKO-2-(3-CF₃-pyridyl) —H —F DKP -2-(3-CF₃-pyridyl) —H —CH₃ DKQ-2-(3-CF₃-pyridyl) —H —CF₃ DKR -2-(3-CF₃-pyridyl) —H —OCH₃ DKS-2-(3-CF₃-pyridyl) —H —OCH₂CH₃ DKT -2-(3-CF₃-pyridyl) —H —OCF₃ DKU-2-(3-CF₃-pyridyl) —H -tert-butyl DKV -2-(3-CF₃-pyridyl) —H -iso-propylDKW -4-(5-chloropyrimidinyl) —Cl —H DKX -4-(5-chloropyrimidinyl) —Br —HDKY -4-(5-chloropyrimidinyl) —F —H DKZ -4-(5-chloropyrimidinyl) —CH₃ —HDLA -4-(5-chloropyrimidinyl) —CF₃ —H DLB -4-(5-chloropyrimidinyl) —OCH₃—H DLC -4-(5-chloropyrimidinyl) —OCH₂CH₃ —H DLD -4-(5-chloropyrimidinyl)—OCF₃ —H DLE -4-(5-chloropyrimidinyl) -tert-butyl —H DLF-4-(5-chloropyrimidinyl) -iso-propyl —H DLG -4-(5-chloropyrimidinyl)—CH₃ —CH₃ DLH -4-(5-chloropyrimidinyl) —H —H DLI-4-(5-chloropyrimidinyl) —H —Cl DLJ -4-(5-chloropyrimidinyl) —H —Br DLK-4-(5-chloropyrimidinyl) —H —F DLL -4-(5-chloropyrimidinyl) —H —CH₃ DLM-4-(5-chloropyrimidinyl) —H —CF₃ DLN -4-(5-chloropyrimidinyl) —H —OCH₃DLO -4-(5-chloropyrimidinyl) —H —OCH₂CH₃ DLP -4-(5-chloropyrimidinyl) —H—OCF₃ DLQ -4-(5-chloropyrimidinyl) —H -tert-butyl DLR-4-(5-chloropyrimidinyl) —H -iso-propyl DLS -4-(5-methylpyrimidinyl) —Cl—H DLT -4-(5-methylpyrimidinyl) —Br —H DLU -4-(5-methylpyrimidinyl) —F—H DLV -4-(5-methylpyrimidinyl) —CH₃ —H DLW -4-(5-methylpyrimidinyl)—CF₃ —H DLX -4-(5-methylpyrimidinyl) —OCH₃ —H DLY-4-(5-methylpyrimidinyl) —OCH₂CH₃ —H DLZ -4-(5-methylpyrimidinyl) —OCF₃—H DMA -4-(5-methylpyrimidinyl) -tert-butyl —H DMB-4-(5-methylpyrimidinyl) -iso-propyl —H DMC -4-(5-methylpyrimidinyl)—CH₃ —CH₃ DMD -4-(5-methylpyrimidinyl) —H —H DME-4-(5-methylpyrimidinyl) —H —Cl DMF -4-(5-methylpyrimidinyl) —H —Br DMG-4-(5-methylpyrimidinyl) —H —F DMH -4-(5-methylpyrimidinyl) —H —CH₃ DMI-4-(5-methylpyrimidinyl) —H —CF₃ DMJ -4-(5-methylpyrimidinyl) —H —OCH₃DMK -4-(5-methylpyrimidinyl) —H —OCH₂CH₃ DML -4-(5-methylpyrimidinyl) —H—OCF₃ DMM -4-(5-methylpyrimidinyl) —H -tert-butyl DMN-4-(5-methylpyrimidinyl) —H -iso-propyl DMO -2-pyrazinyl —Cl —H DMP-2-pyrazinyl —Br —H DMQ -2-pyrazinyl —F —H DMR -2-pyrazinyl —CH₃ —H DMS-2-pyrazinyl —CF₃ —H DMT -2-pyrazinyl —OCH₃ —H DMU -2-pyrazinyl —OCH₂CH₃—H DMV -2-pyrazinyl —OCF₃ —H DMW -2-pyrazinyl -tert-butyl —H DMX-2-pyrazinyl -iso-propyl —H DMY -2-pyrazinyl —CH₃ —CH₃ DMZ -2-pyrazinyl—H —H DNA -2-pyrazinyl —H —Cl DNB -2-pyrazinyl —H —Br DNC -2-pyrazinyl—H —F DND -2-pyrazinyl —H —CH₃ DNE -2-pyrazinyl —H —CF₃ DNF -2-pyrazinyl—H —OCH₃ DNG -2-pyrazinyl —H —OCH₂CH₃ DNH -2-pyrazinyl —H —OCF₃ DNI-2-pyrazinyl —H -tert-butyl DNJ -2-pyrazinyl —H -iso-propyl DNK-2-(3-chloropyrazinyl) —Cl —H DNL -2-(3-chloropyrazinyl) —Br —H DNM-2-(3-chloropyrazinyl) —F —H DNN -2-(3-chloropyrazinyl) —CH₃ —H DNO-2-(3-chloropyrazinyl) —CF₃ —H DNP -2-(3-chloropyrazinyl) —OCH₃ —H DNQ-2-(3-chloropyrazinyl) —OCH₂CH₃ —H DNR -2-(3-chloropyrazinyl) —OCF₃ —HDNS -2-(3-chloropyrazinyl) -tert-butyl —H DNT -2-(3-chloropyrazinyl)-iso-propyl —H DNU -2-(3-chloropyrazinyl) —CH₃ —CH₃ DNV-2-(3-chloropyrazinyl) —H —H DNW -2-(3-chloropyrazinyl) —H —Cl DNX-2-(3-chloropyrazinyl) —H —Br DNY -2-(3-chloropyrazinyl) —H —F DNZ-2-(3-chloropyrazinyl) —H —CH₃ DOA -2-(3-chloropyrazinyl) —H —CF₃ DOB-2-(3-chloropyrazinyl) —H —OCH₃ DOC -2-(3-chloropyrazinyl) —H —OCH₂CH₃DOD -2-(3-chloropyrazinyl) —H —OCF₃ DOE -2-(3-chloropyrazinyl) —H-tert-butyl DOF -2-(3-chloropyrazinyl) —H -iso-propyl DOG-2-(3-methylpyrazinyl) —Cl —H DOH -2-(3-methylpyrazinyl) —Br —H DOI-2-(3-methylpyrazinyl) —F —H DOJ -2-(3-methylpyrazinyl) —CH₃ —H DOK-2-(3-methylpyrazinyl) —CF₃ —H DOL -2-(3-methylpyrazinyl) —OCH₃ —H DOM-2-(3-methylpyrazinyl) —OCH₂CH₃ —H DON -2-(3-methylpyrazinyl) —OCF₃ —HDOO -2-(3-methylpyrazinyl) -tert-butyl —H DOP -2-(3-methylpyrazinyl)-iso-propyl —H DOQ -2-(3-methylpyrazinyl) —CH₃ —CH₃ DOR-2-(3-methylpyrazinyl) —H —H DOS -2-(3-methylpyrazinyl) —H —Cl DOT-2-(3-methylpyrazinyl) —H —Br DOU -2-(3-methylpyrazinyl) —H —F DOV-2-(3-methylpyrazinyl) —H —CH₃ DOW -2-(3-methylpyrazinyl) —H —CF₃ DOX-2-(3-methylpyrazinyl) —H —OCH₃ DOY -2-(3-methylpyrazinyl) —H —OCH₂CH₃DOZ -2-(3-methylpyrazinyl) —H —OCF₃ DPA -2-(3-methylpyrazinyl) —H-tert-butyl DPB -2-(3-methylpyrazinyl) —H -iso-propyl DPC -2-pyridazinyl—Cl —H DPD -2-pyridazinyl —Br —H DPE -2-pyridazinyl —F —H DPF-2-pyridazinyl —CH₃ —H DPG -2-pyridazinyl —CF₃ —H DPH -2-pyridazinyl—OCH₃ —H DPI -2-pyridazinyl —OCH₂CH₃ —H DPJ -2-pyridazinyl —OCF₃ —H DPK-2-pyridazinyl -tert-butyl —H DPL -2-pyridazinyl -iso-propyl —H DPM-2-pyridazinyl —CH₃ —CH₃ DPN -2-pyridazinyl —H —H DPO -2-pyridazinyl —H—Cl DPP -2-pyridazinyl —H —Br DPQ -2-pyridazinyl —H —F DPR-2-pyridazinyl —H —CH₃ DPS -2-pyridazinyl —H —CF₃ DPT -2-pyridazinyl —H—OCH₃ DPU -2-pyridazinyl —H —OCH₂CH₃ DPV -2-pyridazinyl —H —OCF₃ DPW-2-pyridazinyl —H -tert-butyl DPX -2-pyridazinyl —H -iso-propyl DPY-3-(4-chloropyridazinyl) —Cl —H DPZ -3-(4-chloropyridazinyl) —Br —H DQA-3-(4-chloropyridazinyl) —F —H DQB -3-(4-chloropyridazinyl) —CH₃ —H DQC-3-(4-chloropyridazinyl) —CF₃ —H DQD -3-(4-chloropyridazinyl) —OCH₃ —HDQE -3-(4-chloropyridazinyl) —OCH₂CH₃ —H DQF -3-(4-chloropyridazinyl)—OCF₃ —H DQG -3-(4-chloropyridazinyl) -tert-butyl —H DQH-3-(4-chloropyridazinyl) -iso-propyl —H DQI -3-(4-chloropyridazinyl)—CH₃ —CH₃ DQJ -3-(4-chloropyridazinyl) —H —H DQK-3-(4-chloropyridazinyl) —H —Cl DQL -3-(4-chloropyridazinyl) —H —Br DQM-3-(4-chloropyridazinyl) —H —F DQN -3-(4-chloropyridazinyl) —H —CH₃ DQO-3-(4-chloropyridazinyl) —H —CF₃ DQP -3-(4-chloropyridazinyl) —H —OCH₃DQQ -3-(4-chloropyridazinyl) —H —OCH₂CH₃ DQR -3-(4-chloropyridazinyl) —H—OCF₃ DQS -3-(4-chloropyridazinyl) —H -tert-butyl DQT-3-(4-chloropyridazinyl) —H -iso-propyl DQU -3-(4-methylpyridazinyl) —Cl—H DQV -3-(4-methylpyridazinyl) —Br —H DQW -3-(4-methylpyridazinyl) —F—H DQX -3-(4-methylpyridazinyl) —CH₃ —H DQY -3-(4-methylpyridazinyl)—CF₃ —H DQZ -3-(4-methylpyridazinyl) —OCH₃ —H DRA-3-(4-methylpyridazinyl) —OCH₂CH₃ —H DRB -3-(4-methylpyridazinyl) —OCF₃—H DRC -3-(4-methylpyridazinyl) -tert-butyl —H DRD-3-(4-methylpyridazinyl) -iso-propyl —H DRE -3-(4-methylpyridazinyl)—CH₃ —CH₃ DRF -3-(4-methylpyridazinyl) —H —H DRG-3-(4-methylpyridazinyl) —H —Cl DRH -3-(4-methylpyridazinyl) —H —Br DRI-3-(4-methylpyridazinyl) —H —F DRJ -3-(4-methylpyridazinyl) —H —CH₃ DRK-3-(4-methylpyridazinyl) —H —CF₃ DRL -3-(4-methylpyridazinyl) —H —OCH₃DRM -3-(4-methylpyridazinyl) —H —OCH₂CH₃ DRN -3-(4-methylpyridazinyl) —H—OCF₃ DRO -3-(4-methylpyridazinyl) —H -tert-butyl DRP-3-(4-methylpyridazinyl) —H -iso-propyl DRQ -4-thiazanyl —Cl —H DRR-4-thiazanyl —Br —H DRS -4-thiazanyl —F —H DRT -4-thiazanyl —CH₃ —H DRU-4-thiazanyl —CF₃ —H DRV -4-thiazanyl —OCH₃ —H DRW -4-thiazanyl —OCH₂CH₃—H DRX -4-thiazanyl —OCF₃ —H DRY -4-thiazanyl -tert-butyl —H DRZ-4-thiazanyl -iso-propyl —H DSA -4-thiazanyl —CH₃ —CH₃ DSB -4-thiazanyl—H —H DSC -4-thiazanyl —H —Cl DSD -4-thiazanyl —H —Br DSE -4-thiazanyl—H —F DSF -4-thiazanyl —H —CH₃ DSG -4-thiazanyl —H —CF₃ DSH -4-thiazanyl—H —OCH₃ DSI -4-thiazanyl —H —OCH₂CH₃ DSJ -4-thiazanyl —H —OCF₃ DSK-4-thiazanyl —H -tert-butyl DSL -4-thiazanyl —H -iso-propyl DSM-5-(4-chlorothiazanyl) —Cl —H DSN -5-(4-chlorothiazanyl) —Br —H DSO-5-(4-chlorothiazanyl) —F —H DSP -5-(4-chlorothiazanyl) —CH₃ —H DSQ-5-(4-chlorothiazanyl) —CF₃ —H DSR -5-(4-chlorothiazanyl) —OCH₃ —H DSS-5-(4-chlorothiazanyl) —OCH₂CH₃ —H DST -5-(4-chlorothiazanyl) —OCF₃ —HDSU -5-(4-chlorothiazanyl) -tert-butyl —H DSV -5-(4-chlorothiazanyl)-iso-propyl —H DSW -5-(4-chlorothiazanyl) —CH₃ —CH₃ DSX-5-(4-chlorothiazanyl) —H —H DSY -5-(4-chlorothiazanyl) —H —Cl DSZ-5-(4-chlorothiazanyl) —H —Br DTA -5-(4-chlorothiazanyl) —H —F DTB-5-(4-chlorothiazanyl) —H —CH₃ DTC -5-(4-chlorothiazanyl) —H —CF₃ DTD-5-(4-chlorothiazanyl) —H —OCH₃ DTE -5-(4-chlorothiazanyl) —H —OCH₂CH₃DTF -5-(4-chlorothiazanyl) —H —OCF₃ DTG -5-(4-chlorothiazanyl) —H-tert-butyl DTH -5-(4-chlorothiazanyl) —H -iso-propyl DTI-5-(4-methylthiazanyl) —Cl —H DTJ -5-(4-methylthiazanyl) —Br —H DTK-5-(4-methylthiazanyl) —F —H DTL -5-(4-methylthiazanyl) —CH₃ —H DTM-5-(4-methylthiazanyl) —CF₃ —H DTN -5-(4-methylthiazanyl) —OCH₃ —H DTO-5-(4-methylthiazanyl) —OCH₂CH₃ —H DTP -5-(4-methylthiazanyl) —OCF₃ —HDTQ -5-(4-methylthiazanyl) -tert-butyl —H DTR -5-(4-methylthiazanyl)-iso-propyl —H DTS -5-(4-methylthiazanyl) —CH₃ —CH₃ DTT-5-(4-methylthiazanyl) —H —H DTU -5-(4-methylthiazanyl) —H —Cl DTV-5-(4-methylthiazanyl) —H —Br DTW -5-(4-methylthiazanyl) —H —F DTX-5-(4-methylthiazanyl) —H —CH₃ DTY -5-(4-methylthiazanyl) —H —CF₃ DTZ-5-(4-methylthiazanyl) —H —OCH₃ DUA -5-(4-methylthiazanyl) —H —OCH₂CH₃DUB -5-(4-methylthiazanyl) —H —OCF₃ DUC -5-(4-methylthiazanyl) —H-tert-butyl DUD -5-(4-methylthiazanyl) —H -iso-propyl

TABLE XI

and pharmaceutically acceptable salts thereof, wherein: Compound Ar₁ R₈R₉ DUE (a, b, and c) -2-pyridazinyl —Cl —H DUF (a, b, and c)-2-pyridazinyl —Br —H DUG (a, b, and c) -2-pyridazinyl —F —H DUH (a, b,and c) -2-pyridazinyl —CH₃ —H DUI (a, b, and c) -2-pyridazinyl —CF₃ —HDUJ (a, b, and c) -2-pyridazinyl —OCH₃ —H DUK (a, b, and c)-2-pyridazinyl —OCH₂CH₃ —H DUL (a, b, and c) -2-pyridazinyl —OCF₃ —H DUM(a, b, and c) -2-pyridazinyl -tert-butyl —H DUN (a, b, and c)-2-pyridazinyl -iso-propyl —H DUO (a, b, and c) -2-pyridazinyl —CH₃ —CH₃DUP (a, b, and c) -2-pyridazinyl —H —H DUQ (a, b, and c) -2-pyridazinyl—H —Cl DUR (a, b, and c) -2-pyridazinyl —H —Br DUS (a, b, and c)-2-pyridazinyl —H —F DUT (a, b, and c) -2-pyridazinyl —H —CH₃ DUU (a, b,and c) -2-pyridazinyl —H —CF₃ DUV (a, b, and c) -2-pyridazinyl —H —OCH₃DUW (a, b, and c) -2-pyridazinyl —H —OCH₂CH₃ DUX (a, b, and c)-2-pyridazinyl —H —OCF₃ DUY (a, b, and c) -2-pyridazinyl —H -tert-butylDUZ (a, b, and c) -2-pyridazinyl —H -iso-propyl DVA (a, b, and c)-3-(4-chloropyridazinyl) —Cl —H DVB (a, b, and c)-3-(4-chloropyridazinyl) —Br —H DVC (a, b, and c)-3-(4-chloropyridazinyl) —F —H DVD (a, b, and c)-3-(4-chloropyridazinyl) —CH₃ —H DVE (a, b, and c)-3-(4-chloropyridazinyl) —CF₃ —H DVF (a, b, and c)-3-(4-chloropyridazinyl) —OCH₃ —H DVG (a, b, and c)-3-(4-chloropyridazinyl) —OCH₂CH₃ —H DVH (a, b, and c)-3-(4-chloropyridazinyl) —OCF₃ —H DVI (a, b, and c)-3-(4-chloropyridazinyl) -tert-butyl —H DVJ (a, b, and c)-3-(4-chloropyridazinyl) -iso-propyl —H DVK (a, b, and c)-3-(4-chloropyridazinyl) —CH₃ —CH₃ DVL (a, b, and c)-3-(4-chloropyridazinyl) —H —H DVM (a, b, and c)-3-(4-chloropyridazinyl) —H —Cl DVN (a, b, and c)-3-(4-chloropyridazinyl) —H —Br DVO (a, b, and c)-3-(4-chloropyridazinyl) —H —F DVP (a, b, and c)-3-(4-chloropyridazinyl) —H —CH₃ DVQ (a, b, and c)-3-(4-chloropyridazinyl) —H —CF₃ DVR (a, b, and c)-3-(4-chloropyridazinyl) —H —OCH₃ DVS (a, b, and c)-3-(4-chloropyridazinyl) —H —OCH₂CH₃ DVT (a, b, and c)-3-(4-chloropyridazinyl) —H —OCF₃ DVU (a, b, and c)-3-(4-chloropyridazinyl) —H -tert-butyl DVV (a, b, and c)-3-(4-chloropyridazinyl) —H -iso-propyl DVW (a, b, and c)-3-(4-methylpyridazinyl) —Cl —H DVX (a, b, and c)-3-(4-methylpyridazinyl) —Br —H DVY (a, b, and c)-3-(4-methylpyridazinyl) —F —H DVZ (a, b, and c)-3-(4-methylpyridazinyl) —CH₃ —H DWA (a, b, and c)-3-(4-methylpyridazinyl) —CF₃ —H DWB (a, b, and c)-3-(4-methylpyridazinyl) —OCH₃ —H DWC (a, b, and c)-3-(4-methylpyridazinyl) —OCH₂CH₃ —H DWD (a, b, and c)-3-(4-methylpyridazinyl) —OCF₃ —H DWE (a, b, and c)-3-(4-methylpyridazinyl) -tert-butyl —H DWF (a, b, and c)-3-(4-methylpyridazinyl) -iso-propyl —H DWG (a, b, and c)-3-(4-methylpyridazinyl) —CH₃ —CH₃ DWH (a, b, and c)-3-(4-methylpyridazinyl) —H —H DWI (a, b, and c)-3-(4-methylpyridazinyl) —H —Cl DWJ (a, b, and c)-3-(4-methylpyridazinyl) —H —Br DWK (a, b, and c)-3-(4-methylpyridazinyl) —H —F DWL (a, b, and c)-3-(4-methylpyridazinyl) —H —CH₃ DWM (a, b, and c)-3-(4-methylpyridazinyl) —H —CF₃ DWN (a, b, and c)-3-(4-methylpyridazinyl) —H —OCH₃ DWO (a, b, and c)-3-(4-methylpyridazinyl) —H —OCH₂CH₃ DWP (a, b, and c)-3-(4-methylpyridazinyl) —H —OCF₃ DWQ (a, b, and c)-3-(4-methylpyridazinyl) —H -tert-butyl DWR (a, b, and c)-3-(4-methylpyridazinyl) —H -iso-propyl DWS (a, b, and c) -4-thiazanyl—Cl —H DWT (a, b, and c) -4-thiazanyl —Br —H DWU (a, b, and c)-4-thiazanyl —F —H DWV (a, b, and c) -4-thiazanyl —CH₃ —H DWW (a, b, andc) -4-thiazanyl —CF₃ —H DWX (a, b, and c) -4-thiazanyl —OCH₃ —H DWY (a,b, and c) -4-thiazanyl —OCH₂CH₃ —H DWZ (a, b, and c) -4-thiazanyl —OCF₃—H DXA (a, b, and c) -4-thiazanyl -tert-butyl —H DXB (a, b, and c)-4-thiazanyl -iso-propyl —H DXC (a, b, and c) -4-thiazanyl —CH₃ —CH₃ DXD(a, b, and c) -4-thiazanyl —H —H DXE (a, b, and c) -4-thiazanyl —H —ClDXF (a, b, and c) -4-thiazanyl —H —Br DXG (a, b, and c) -4-thiazanyl —H—F DXH (a, b, and c) -4-thiazanyl —H —CH₃ DXI (a, b, and c) -4-thiazanyl—H —CF₃ DXJ (a, b, and c) -4-thiazanyl —H —OCH₃ DXK (a, b, and c)-4-thiazanyl —H —OCH₂CH₃ DXL (a, b, and c) -4-thiazanyl —H —OCF₃ DXM (a,b, and c) -4-thiazanyl —H -tert-butyl DXN (a, b, and c) -4-thiazanyl —H-iso-propyl DXO (a, b, and c) -5-(4-chlorothiazanyl) —Cl —H DXP (a, b,and c) -5-(4-chlorothiazanyl) —Br —H DXQ (a, b, and c)-5-(4-chlorothiazanyl) —F —H DXR (a, b, and c) -5-(4-chlorothiazanyl)—CH₃ —H DXS (a, b, and c) -5-(4-chlorothiazanyl) —CF₃ —H DXT (a, b, andc) -5-(4-chlorothiazanyl) —OCH₃ —H DXU (a, b, and c)-5-(4-chlorothiazanyl) —OCH₂CH₃ —H DXV (a, b, and c)-5-(4-chlorothiazanyl) —OCF₃ —H DXW (a, b, and c) -5-(4-chlorothiazanyl)-tert-butyl —H DXX (a, b, and c) -5-(4-chlorothiazanyl) -iso-propyl —HDXY (a, b, and c) -5-(4-chlorothiazanyl) —CH₃ —CH₃ DXZ (a, b, and c)-5-(4-chlorothiazanyl) —H —H DYA (a, b, and c) -5-(4-chlorothiazanyl) —H—Cl DYB (a, b, and c) -5-(4-chlorothiazanyl) —H —Br DYC (a, b, and c)-5-(4-chlorothiazanyl) —H —F DYD (a, b, and c) -5-(4-chlorothiazanyl) —H—CH₃ DYE (a, b, and c) -5-(4-chlorothiazanyl) —H —CF₃ DYE (a, b, and c)-5-(4-chlorothiazanyl) —H —OCH₃ DYG (a, b, and c) -5-(4-chlorothiazanyl)—H —OCH₂CH₃ DYH (a, b, and c) -5-(4-chlorothiazanyl) —H —OCF₃ DYI (a, b,and c) -5-(4-chlorothiazanyl) —H -tert-butyl DYJ (a, b, and c)-5-(4-chlorothiazanyl) —H -iso-propyl DYK (a, b, and c)-5-(4-methylthiazanyl) —Cl —H DYL (a, b, and c) -5-(4-methylthiazanyl)—Br —H DYM (a, b, and c) -5-(4-methylthiazanyl) —F —H DYN (a, b, and c)-5-(4-methylthiazanyl) —CH₃ —H DYO (a, b, and c) -5-(4-methylthiazanyl)—CF₃ —H DYP (a, b, and c) -5-(4-methylthiazanyl) —OCH₃ —H DYQ (a, b, andc) -5-(4-methylthiazanyl) —OCH₂CH₃ —H DYR (a, b, and c)-5-(4-methylthiazanyl) —OCF₃ —H DYS (a, b, and c) -5-(4-methylthiazanyl)-tert-butyl —H DYT (a, b, and c) -5-(4-methylthiazanyl) -iso-propyl —HDYU (a, b, and c) -5-(4-methylthiazanyl) —CH₃ —CH₃ DYV (a, b, and c)-5-(4-methylthiazanyl) —H —H DYW (a, b, and c) -5-(4-methylthiazanyl) —H—Cl DYX (a, b, and c) -5-(4-methylthiazanyl) —H —Br DYY (a, b, and c)-5-(4-methylthiazanyl) —H —F DYZ (a, b, and c) -5-(4-methylthiazanyl) —H—CH₃ DZA (a, b, and c) -5-(4-methylthiazanyl) —H —CF₃ DZB (a, b, and c)-5-(4-methylthiazanyl) —H —OCH₃ DZC (a, b, and c) -5-(4-methylthiazanyl)—H —OCH₂CH₃ DZD (a, b, and c) -5-(4-methylthiazanyl) —H —OCF₃ DZE (a, b,and c) -5-(4-methylthiazanyl) —H -tert-butyl DZF (a, b, and c)-5-(4-methylthiazanyl) —H -iso-propyl “a” means theBenzoazolylpiperazine Compound is racemic. “b” means the carbon atom ofthe piperazine ring attached to the methyl group is in the Rconfiguration. “c” means the carbon atom of the piperazine ring attachedto the methyl group is in the S configuration.

TABLE XII

and pharmaceutically acceptable salts thereof, wherein: Compound Ar₁ R₈R₉ DZG (a, b, and c) -2-(3-chloropyridyl) —Cl —H DZH (a, b, and c)-2-(3-chloropyridyl) —Br —H DZI (a, b, and c) -2-(3-chloropyridyl) —F —HDZJ (a, b, and c) -2-(3-chloropyridyl) —CH₃ —H DZK (a, b, and c)-2-(3-chloropyridyl) —CF₃ —H DZL (a, b, and c) -2-(3-chloropyridyl)—OCH₃ —H DZM (a, b, and c) -2-(3-chloropyridyl) —OCH₂CH₃ —H DZN (a, b,and c) -2-(3-chloropyridyl) —OCF₃ —H DZO (a, b, and c)-2-(3-chloropyridyl) -tert-butyl —H DZP (a, b, and c)-2-(3-chloropyridyl) -iso-propyl —H DZQ (a, b, and c)-2-(3-chloropyridyl) —CH₃ —CH₃ DZR (a, b, and c) -2-(3-chloropyridyl) —H—H DZS (a, b, and c) -2-(3-chloropyridyl) —H —Cl DZT (a, b, and c)-2-(3-chloropyridyl) —H —Br DZU (a, b, and c) -2-(3-chloropyridyl) —H —FDZV (a, b, and c) -2-(3-chloropyridyl) —H —CH₃ DZW (a, b, and c)-2-(3-chloropyridyl) —H —CF₃ DZX (a, b, and c) -2-(3-chloropyridyl) —H—OCH₃ DZY (a, b, and c) -2-(3-chloropyridyl) —H —OCH₂CH₃ DZZ (a, b, andc) -2-(3-chloropyridyl) —H —OCF₃ EAA (a, b, and c) -2-(3-chloropyridyl)—H -tert-butyl EAB (a, b, and c) -2-(3-chloropyridyl) —H -iso-propyl EAC(a, b, and c) -2-(3-methylpyridyl) —Cl —H EAD (a, b, and c)-2-(3-methylpyridyl) —Br —H EAB (a, b, and c) -2-(3-methylpyridyl) —F —HEAF (a, b, and c) -2-(3-methylpyridyl) —CH₃ —H EAG (a, b, and c)-2-(3-methylpyridyl) —CF₃ —H EAH (a, b, and c) -2-(3-methylpyridyl)—OCH₃ —H EMI (a, b, and c) -2-(3-methylpyridyl) —OCH₂CH₃ —H EMJ (a, b,and c) -2-(3-methylpyridyl) —OCF₃ —H EAK (a, b, and c)-2-(3-methylpyridyl) -tert-butyl —H EAL (a, b, and c)-2-(3-methylpyridyl) -iso-propyl —H EAM (a, b, and c)-2-(3-methylpyridyl) —CH₃ —CH₃ EAN (a, b, and c) -2-(3-methylpyridyl) —H—H EAO (a, b, and c) -2-(3-methylpyridyl) —H —Cl EAP (a, b, and c)-2-(3-methylpyridyl) —H —Br EAQ (a, b, and c) -2-(3-methylpyridyl) —H —FEAR (a, b, and c) -2-(3-methylpyridyl) —H —CH₃ EAS (a, b, and c)-2-(3-methylpyridyl) —H —CF₃ EAT (a, b, and c) -2-(3-methylpyridyl) —H—OCH₃ EAU (a, b, and c) -2-(3-methylpyridyl) —H —OCH₂CH₃ EAV (a, b, andc) -2-(3-methylpyridyl) —H —OCF₃ EAW (a, b, and c) -2-(3-methylpyridyl)—H -tert-butyl EAX (a, b, and c) -2-(3-methylpyridyl) —H -iso-propyl EAY(a, b, and c) -2-(3—CF₃-pyridyl) —Cl —H EAZ (a, b, and c)-2-(3—CF₃-pyridyl) —Br —H EBA (a, b, and c) -2-(3—CF₃-pyridyl) —F —H EBB(a, b, and c) -2-(3—CF₃-pyridyl) —CH₃ —H EBC (a, b, and c)-2-(3—CF₃-pyridyl) —CF₃ —H EBD (a, b, and c) -2-(3—CF₃-pyridyl) —OCH₃ —HEBE (a, b, and c) -2-(3—CF₃-pyridyl) —OCH₂CH₃ —H EBF (a, b, and c)-2-(3—CF₃-pyridyl) —OCF₃ —H EBG (a, b, and c) -2-(3—CF₃-pyridyl)-tert-butyl —H EBH (a, b, and c) -2-(3—CF₃-pyridyl) -iso-propyl —H EBI(a, b, and c) -2-(3—CF₃-pyridyl) —CH₃ —CH₃ EBJ (a, b, and c)-2-(3—CF₃-pyridyl) —H —H EBK (a, b, and c) -2-(3—CF₃-pyridyl) —H —Cl EBL(a, b, and c) -2-(3—CF₃-pyridyl) —H —Br EBM (a, b, and c)-2-(3—CF₃-pyridyl) —H —F EBN (a, b, and c) -2-(3—CF₃-pyridyl) —H —CH₃EBO (a, b, and c) -2-(3—CF₃-pyridyl) —H —CF₃ EBP (a, b, and c)-2-(3—CF₃-pyridyl) —H —OCH₃ EBQ (a, b, and c) -2-(3—CF₃-pyridyl) —H—OCH₂CH₃ EBR (a, b, and c) -2-(3—CF₃-pyridyl) —H —OCF₃ EBS (a, b, and c)-2-(3—CF₃-pyridyl) —H -tert-butyl EBT (a, b, and c) -2-(3—CF₃-pyridyl)—H -iso-propyl EBU (a, b, and c) -4-(5-chloropyrimidinyl) —Cl —H EBV (a,b, and c) -4-(5-chloropyrimidinyl) —Br —H EBW (a, b, and c)-4-(5-chloropyrimidinyl) —F —H EBX (a, b, and c)-4-(5-chloropyrimidinyl) —CH₃ —H EBY (a, b, and c)-4-(5-chloropyrimidinyl) —CF₃ —H EBZ (a, b, and c)-4-(5-chloropyrimidinyl) —OCH₃ —H ECA (a, b, and c)-4-(5-chloropyrimidinyl) —OCH₂CH₃ —H ECB (a, b, and c)-4-(5-chloropyrimidinyl) —OCF₃ —H ECC (a, b, and c)-4-(5-chloropyrimidinyl) -tert-butyl —H ECD (a, b, and c)-4-(5-chloropyrimidinyl) -iso-propyl —H ECE (a, b, and c)-4-(5-chloropyrimidinyl) —CH₃ —CH₃ ECF (a, b, and c)-4-(5-chloropyrimidinyl) —H —H ECG (a, b, and c)-4-(5-chloropyrimidinyl) —H —Cl ECH (a, b, and c)-4-(5-chloropyrimidinyl) —H —Br ECI (a, b, and c)-4-(5-chloropyrimidinyl) —H —F ECJ (a, b, and c)-4-(5-chloropyrimidinyl) —H —CH₃ ECK (a, b, and c)-4-(5-chloropyrimidinyl) —H —CF₃ ECL (a, b, and c)-4-(5-chloropyrimidinyl) —H —OCH₃ ECM (a, b, and c)-4-(5-chloropyrimidinyl) —H —OCH₂CH₃ ECN (a, b, and c)-4-(5-chloropyrimidinyl) —H —OCF₃ ECO (a, b, and c)-4-(5-chloropyrimidinyl) —H -tert-butyl ECP (a, b, and c)-4-(5-chloropyrimidinyl) —H -iso-propyl ECQ (a, b, and c)-4-(5-methylpyrimidinyl) —Cl —H ECR (a, b, and c)-4-(5-methylpyrimidinyl) —Br —H ECS (a, b, and c)-4-(5-methylpyrimidinyl) —F —H ECT (a, b, and c)-4-(5-methylpyrimidinyl) —CH₃ —H ECU (a, b, and c)-4-(5-methylpyrimidinyl) —CF₃ —H ECV (a, b, and c)-4-(5-methylpyrimidinyl) —OCH₃ —H ECW (a, b, and c)-4-(5-methylpyrimidinyl) —OCH₂CH₃ —H ECX (a, b, and c)-4-(5-methylpyrimidinyl) —OCF₃ —H ECY (a, b, and c)-4-(5-methylpyrimidinyl) -tert-butyl —H ECZ (a, b, and c)-4-(5-methylpyrimidinyl) -iso-propyl —H EDA (a, b, and c)-4-(5-methylpyrimidinyl) —CH₃ —CH₃ EDB (a, b, and c)-4-(5-methylpyrimidinyl) —H —H EDC (a, b, and c)-4-(5-methylpyrimidinyl) —H —Cl EDD (a, b, and c)-4-(5-methylpyrimidinyl) —H —Br EDE (a, b, and c)-4-(5-methylpyrimidinyl) —H —F EDF (a, b, and c)-4-(5-methylpyrimidinyl) —H —CH₃ EDG (a, b, and c)-4-(5-methylpyrimidinyl) —H —CF₃ EDH (a, b, and c)-4-(5-methylpyrimidinyl) —H —OCH₃ EDI (a, b, and c)-4-(5-methylpyrimidinyl) —H —OCH₂CH₃ EDJ (a, b, and c)-4-(5-methylpyrimidinyl) —H —OCF₃ EDK (a, b, and c)-4-(5-methylpyrimidinyl) —H -tert-butyl EDL (a, b, and c)-4-(5-methylpyrimidinyl) —H -iso-propyl EDM (a, b, and c) -2-pyrazinyl—Cl —H EDN (a, b, and c) -2-pyrazinyl —Br —H EDO (a, b, and c)-2-pyrazinyl —F —H EDP (a, b, and c) -2-pyrazinyl —CH₃ —H EDQ (a, b, andc) -2-pyrazinyl —CF₃ —H EDR (a, b, and c) -2-pyrazinyl —OCH₃ —H EDS (a,b, and c) -2-pyrazinyl —OCH₂CH₃ —H EDT (a, b, and c) -2-pyrazinyl —OCF₃—H EDU (a, b, and c) -2-pyrazinyl -tert-butyl —H EDV (a, b, and c)-2-pyrazinyl -iso-propyl —H EDW (a, b, and c) -2-pyrazinyl —CH₃ —CH₃ EDX(a, b, and c) -2-pyrazinyl —H —H EDY (a, b, and c) -2-pyrazinyl —H —ClEDZ (a, b, and c) -2-pyrazinyl —H —Br EEA (a, b, and c) -2-pyrazinyl —H—F EEB (a, b, and c) -2-pyrazinyl —H —CH₃ EEC (a, b, and c) -2-pyrazinyl—H —CF₃ EED (a, b, and c) -2-pyrazinyl —H —OCH₃ EEE (a, b, and c)-2-pyrazinyl —H —OCH₂CH₃ EEF (a, b, and c) -2-pyrazinyl —H —OCF₃ EEG (a,b, and c) -2-pyrazinyl —H -tert-butyl EEH (a, b, and c) -2-pyrazinyl —H-iso-propyl EEI (a, b, and c) -2-(3-chloropyrazinyl) —Cl —H EEJ (a, b,and c) -2-(3-chloropyrazinyl) —Br —H EEK (a, b, and c)-2-(3-chloropyrazinyl) —F —H EEL (a, b, and c) -2-(3-chloropyrazinyl)—CH₃ —H EEM (a, b, and c) -2-(3-chloropyrazinyl) —CF₃ —H EEN (a, b, andc) -2-(3-chloropyrazinyl) —OCH₃ —H EEO (a, b, and c)-2-(3-chloropyrazinyl) —OCH₂CH₃ —H EEP (a, b, and c)-2-(3-chloropyrazinyl) —OCF₃ —H EEQ (a, b, and c) -2-(3-chloropyrazinyl)-tert-butyl —H EER (a, b, and c) -2-(3-chloropyrazinyl) -iso-propyl —HEES (a, b, and c) -2-(3-chloropyrazinyl) —CH₃ —CH₃ EET (a, b, and c)-2-(3-chloropyrazinyl) —H —H EEU (a, b, and c) -2-(3-chloropyrazinyl) —H—Cl EEV (a, b, and c) -2-(3-chloropyrazinyl) —H —Br EEW (a, b, and c)-2-(3-chloropyrazinyl) —H —F EEX (a, b, and c) -2-(3-chloropyrazinyl) —H—CH₃ EEY (a, b, and c) -2-(3-chloropyrazinyl) —H —CF₃ EEZ (a, b, and c)-2-(3-chloropyrazinyl) —H —OCH₃ EFA (a, b, and c) -2-(3-chloropyrazinyl)—H —OCH₂CH₃ EFB (a, b, and c) -2-(3-chloropyrazinyl) —H —OCF₃ EFC (a, b,and c) -2-(3-chloropyrazinyl) —H -tert-butyl EFD (a, b, and c)-2-(3-chloropyrazinyl) —H -iso-propyl EFE (a, b, and c)-2-(3-methylpyrazinyl) —Cl —H EFF (a, b, and c) -2-(3-methylpyrazinyl)—Br —H EFG (a, b, and c) -2-(3-methylpyrazinyl) —F —H EFH (a, b, and c)-2-(3-methylpyrazinyl) —CH₃ —H EFI (a, b, and c) -2-(3-methylpyrazinyl)—CF₃ —H EFJ (a, b, and c) -2-(3-methylpyrazinyl) —OCH₃ —H EFK (a, b, andc) -2-(3-methylpyrazinyl) —OCH₂CH₃ —H EFL (a, b, and c)-2-(3-methylpyrazinyl) —OCF₃ —H EFM (a, b, and c) -2-(3-methylpyrazinyl)-tert-butyl —H EFN (a, b, and c) -2-(3-methylpyrazinyl) -iso-propyl —HEFO (a, b, and c) -2-(3-methylpyrazinyl) —CH₃ —CH₃ EFP (a, b, and c)-2-(3-methylpyrazinyl) —H —H EFQ (a, b, and c) -2-(3-methylpyrazinyl) —H—Cl EFR (a, b, and c) -2-(3-methylpyrazinyl) —H —Br EFS (a, b, and c)-2-(3-methylpyrazinyl) —H —F EFT (a, b, and c) -2-(3-methylpyrazinyl) —H—CH₃ EFU (a, b, and c) -2-(3-methylpyrazinyl) —H —CF₃ EFV (a, b, and c)-2-(3-methylpyrazinyl) —H —OCH₃ EFW (a, b, and c) -2-(3-methylpyrazinyl)—H —OCH₂CH₃ EFX (a, b, and c) -2-(3-methylpyrazinyl) —H —OCF₃ EFY (a, b,and c) -2-(3-methylpyrazinyl) —H -tert-butyl EFZ (a, b, and c)-2-(3-methylpyrazinyl) —H -iso-propyl EGA (a, b, and c) -2-pyridazinyl—Cl —H EGB (a, b, and c) -2-pyridazinyl —Br —H EGC (a, b, and c)-2-pyridazinyl —F —H EGD (a, b, and c) -2-pyridazinyl —CH₃ —H EGE (a, b,and c) -2-pyridazinyl —CF₃ —H EGF (a, b, and c) -2-pyridazinyl —OCH₃ —HEGG (a, b, and c) -2-pyridazinyl —OCH₂CH₃ —H EGH (a, b, and c)-2-pyridazinyl —OCF₃ —H EGI (a, b, and c) -2-pyridazinyl -tert-butyl —HEGJ (a, b, and c) -2-pyridazinyl -iso-propyl —H EGK (a, b, and c)-2-pyridazinyl —CH₃ —CH₃ EGL (a, b, and c) -2-pyridazinyl —H —H EGM (a,b, and c) -2-pyridazinyl —H —Cl EGN (a, b, and c) -2-pyridazinyl —H —BrEGO (a, b, and c) -2-pyridazinyl —H —F EGP (a, b, and c) -2-pyridazinyl—H —CH₃ EGQ (a, b, and c) -2-pyridazinyl —H —CF₃ EGR (a, b, and c)-2-pyridazinyl —H —OCH₃ EGS (a, b, and c) -2-pyridazinyl —H —OCH₂CH₃ EGT(a, b, and c) -2-pyridazinyl —H —OCF₃ EGU (a, b, and c) -2-pyridazinyl—H -tert-butyl EGV (a, b, and c) -2-pyridazinyl —H -iso-propyl EGW (a,b, and c) -3-(4-chloropyridazinyl) —Cl —H EGX (a, b, and c)-3-(4-chloropyridazinyl) —Br —H EGY (a, b, and c)-3-(4-chloropyridazinyl) —F —H EGZ (a, b, and c)-3-(4-chloropyridazinyl) —CH₃ —H EHA (a, b, and c)-3-(4-chloropyridazinyl) —CF₃ —H EHB (a, b, and c)-3-(4-chloropyridazinyl) —OCH₃ —H EHC (a, b, and c)-3-(4-chloropyridazinyl) —OCH₂CH₃ —H EHD (a, b, and c)-3-(4-chloropyridazinyl) —OCF₃ —H EHE (a, b, and c)-3-(4-chloropyridazinyl) -tert-butyl —H EHF (a, b, and c)-3-(4-chloropyridazinyl) -iso-propyl —H EHG (a, b, and c)-3-(4-chloropyridazinyl) —CH₃ —CH₃ EHH (a, b, and c)-3-(4-chloropyridazinyl) —H —H EHI (a, b, and c)-3-(4-chloropyridazinyl) —H —Cl EHJ (a, b, and c)-3-(4-chloropyridazinyl) —H —Br EHK (a, b, and c)-3-(4-chloropyridazinyl) —H —F EHL (a, b, and c)-3-(4-chloropyridazinyl) —H —CH₃ EHM (a, b, and c)-3-(4-chloropyridazinyl) —H —CF₃ EHN (a, b, and c)-3-(4-chloropyridazinyl) —H —OCH₃ EHO (a, b, and c)-3-(4-chloropyridazinyl) —H —OCH₂CH₃ EHP (a, b, and c)-3-(4-chloropyridazinyl) —H —OCF₃ EHQ (a, b, and c)-3-(4-chloropyridazinyl) —H -tert-butyl EHR (a, b, and c)-3-(4-chloropyridazinyl) —H -iso-propyl EHS (a, b, and c)-3-(4-methylpyridazinyl) —Cl —H EHT (a, b, and c)-3-(4-methylpyridazinyl) —Br —H EHU (a, b, and c)-3-(4-methylpyridazinyl) —F —H EHV (a, b, and c)-3-(4-methylpyridazinyl) —CH₃ —H EHW (a, b, and c)-3-(4-methylpyridazinyl) —CF₃ —H EHX (a, b, and c)-3-(4-methylpyridazinyl) —OCH₃ —H EHY (a, b, and c)-3-(4-methylpyridazinyl) —OCH₂CH₃ —H EHZ (a, b, and c)-3-(4-methylpyridazinyl) —OCF₃ —H EIA (a, b, and c)-3-(4-methylpyridazinyl) -tert-butyl —H EIB (a, b, and c)-3-(4-methylpyridazinyl) -iso-propyl —H EIC (a, b, and c)-3-(4-methylpyridazinyl) —CH₃ —CH₃ EID (a, b, and c)-3-(4-methylpyridazinyl) —H —H EIE (a, b, and c)-3-(4-methylpyridazinyl) —H —Cl EIF (a, b, and c)-3-(4-methylpyridazinyl) —H —Br EIG (a, b, and c)-3-(4-methylpyridazinyl) —H —F EIH (a, b, and c)-3-(4-methylpyridazinyl) —H —CH₃ EII (a, b, and c)-3-(4-methylpyridazinyl) —H —CF₃ EIJ (a, b, and c)-3-(4-methylpyridazinyl) —H —OCH₃ EIK (a, b, and c)-3-(4-methylpyridazinyl) —H —OCH₂CH₃ EIL (a, b, and c)-3-(4-methylpyridazinyl) —H —OCF₃ EIM (a, b, and c)-3-(4-methylpyridazinyl) —H -tert-butyl EIN (a, b, and c)-3-(4-methylpyridazinyl) —H -iso-propyl EIO (a, b, and c) -4-thiazanyl—Cl —H EIP (a, b, and c) -4-thiazanyl —Br —H EIQ (a, b, and c)-4-thiazanyl —F —H EIR (a, b, and c) -4-thiazanyl —CH₃ —H EIS (a, b, andc) -4-thiazanyl —CF₃—H EIT (a, b, and c) -4-thiazanyl —OCH₃ —H EIU (a,b, and c) -4-thiazanyl —OCH₂CH₃ —H EIV (a, b, and c) -4-thiazanyl —OCF₃—H EIW (a, b, and c) -4-thiazanyl -tert-butyl —H EIX (a, b, and c)-4-thiazanyl -iso-propyl —H EIY (a, b, and c) -4-thiazanyl —CH₃ —CH₃ EIZ(a, b, and c) -4-thiazanyl —H —H EJA (a, b, and c) -4-thiazanyl —H —ClEJB (a, b, and c) -4-thiazanyl —H —Br EJC (a, b, and c) -4-thiazanyl —H—F EJD (a, b, and c) -4-thiazanyl —H —CH₃ EJE (a, b, and c) -4-thiazanyl—H —CF₃ EJF (a, b, and c) -4-thiazanyl —H —OCH₃ EJG (a, b, and c)-4-thiazanyl —H —OCH₂CH₃ EJH (a, b, and c) -4-thiazanyl —H —OCF₃ EJI (a,b, and c) -4-thiazanyl —H -tert-butyl EJJ (a, b, and c) -4-thiazanyl —H-iso-propyl EJK (a, b, and c) -5-(4-chlorothiazanyl) —Cl —H EJL (a, b,and c) -5-(4-chlorothiazanyl) —Br —H EJM (a, b, and c)-5-(4-chlorothiazanyl) —F —H EJN (a, b, and c) -5-(4-chlorothiazanyl)—CH₃ —H EJO (a, b, and c) -5-(4-chlorotbiazanyl) —CF₃ —H EJP (a, b, andc) -5-(4-chlorothiazanyl) —OCH₃ —H EJQ (a, b, and c)-5-(4-chlorothiazanyl) —OCH₂CH₃ —H EJR (a, b, and c)-5-(4-chlorothiazanyl) —OCF₃ —H EJS (a, b, and c) -5-(4-chlorothiazanyl)-tert-butyl —H EJT (a, b, and c) -5-(4-chlorothiazanyl) -iso-propyl —HEJU (a, b, and c) -5-(4-chlorothiazanyl) —CH₃ —CH₃ EJV (a, b, and c)-5-(4-chlorothiazanyl) —H —H EJW (a, b, and c) -5-(4-chlorothiazanyl) —H—Cl EJX (a, b, and c) -5-(4-chlorothiazanyl) —H —Br EJY (a, b, and c)-5-(4-chlorothiazanyl) —H —F EJZ (a, b, and c) -5-(4-chlorothiazanyl) —H—CH₃ EKA (a, b, and c) -5-(4-chlorothiazanyl) —H —CF₃ EKB (a, b, and c)-5-(4-chlorothiazanyl) —H —OCH₃ EKC (a, b, and c) -5-(4-chlorothiazanyl)—H —OCH₂CH₃ EKD (a, b, and c) -5-(4-chlorothiazanyl) —H —OCF₃ EKE (a, b,and c) -5-(4-chlorothiazanyl) —H -tert-butyl EKF (a, b, and c)-5-(4-chlorothiazanyl) —H -iso-propyl EKG (a, b, and c)-5-(4-methylthiazanyl) —Cl —H EKH (a, b, and c) -5-(4-methylthiazanyl)—Br —H EKI (a, b, and c) -5-(4-methylthiazanyl) —F —H EKJ (a, b, and c)-5-(4-methylthiazanyl) —CH₃ —H EKK (a, b, and c) -5-(4-methylthiazanyl)—CF₃ —H EKL (a, b, and c) -5-(4-methylthiazanyl) —OCH₃ —H EKM (a, b, andc) -5-(4-methylthiazanyl) —OCH₂CH₃ —H EKN (a, b, and c)-5-(4-methylthiazanyl) —OCF₃ —H EKO (a, b, and c) -5-(4-methylthiazanyl)-tert-butyl —H EKP (a, b, and c) -5-(4-methylthiazanyl) -iso-propyl —HEKQ (a, b, and c) -5-(4-methylthiazanyl) —CH₃ —CH₃ EKR (a, b, and c)-5-(4-methylthiazanyl) —H —H EKS (a, b, and c) -5-(4-methylthiazanyl) —H—Cl EKT (a, b, and c) -5-(4-methylthiazanyl) —H —Br EKU (a, b, and c)-5-(4-methylthiazanyl) —H —F EKV (a, b, and c) -5-(4-methylthiazanyl) —H—CH₃ EKW (a, b, and c) -5-(4-methylthiazanyl) —H —CF₃ EKX (a, b, and c)-5-(4-methylthiazanyl) —H —OCH₃ EKY (a, b, and c) -5-(4-methylthiazanyl)—H —OCH₂CH₃ EKZ (a, b, and c) -5-(4-methylthiazanyl) —H —OCF₃ ELA (a, b,and c) -5-(4-methylthiazanyl) —H -tert-butyl ELB (a, b, and c)-5-(4-methylthiazanyl) —H -iso-propyl “a” means theBenzoazolylpiperazine Compound is racemic. “b” means the carbon atom ofthe piperazine ring attached to the methyl group is in the Rconfiguration. “c” means the carbon atom of the piperazine ring attachedto the methyl group is in the S configuration.

TABLE XIII

and pharmaceutically acceptable salts thereof, wherein: Compound Ar₁ R₈B₉ ELC -2-(3-chloropyridyl) —Cl —H ELD -2-(3-chloropyridyl) —Br —H ELE-2-(3-chloropyridyl) —F —H ELF -2-(3-chloropyridyl) —CH₃ —H ELG-2-(3-chloropyridyl) —CF₃ —H ELH -2-(3-chloropyridyl) —OCH₃ —H ELI-2-(3-chloropyridyl) —OCH₂CH₃ —H ELJ -2-(3-chloropyridyl) —OCF₃ —H ELK-2-(3-chloropyridyl) -tert-butyl —H ELL -2-(3-chloropyridyl) -iso-propyl—H ELM -2-(3-chloropyridyl) —CH₃ —CH₃ ELN -2-(3-chloropyridyl) —H —H ELO-2-(3-chloropyridyl) —H —Cl ELP -2-(3-chloropyridyl) —H —Br ELQ-2-(3-chloropyridyl) —H —F ELR -2-(3-chloropyridyl) —H —CH₃ ELS-2-(3-chloropyridyl) —H —CF₃ ELT -2-(3-chloropyridyl) —H —OCH₃ ELU-2-(3-chloropyridyl) —H —OCH₂CH₃ ELV -2-(3-chloropyridyl) —H —OCF₃ ELW-2-(3-chloropyridyl) —H -tert-butyl ELX -2-(3-chloropyridyl) —H-iso-propyl ELY -2-(3-methylpyridyl) —Cl —H ELZ -2-(3-methylpyridyl) —Br—H EMA -2-(3-methylpyridyl) —F —H EMB -2-(3-methylpyridyl) —CH₃ —H EMC-2-(3-methylpyridyl) —CF₃ —H EMD -2-(3-methylpyridyl) —OCH₃ —H EME-2-(3-methylpyridyl) —OCH₂CH₃ —H EMF -2-(3-methylpyridyl) —OCF₃ —H EMG-2-(3-methylpyridyl) -tert-butyl —H EMH -2-(3-methylpyridyl) -iso-propyl—H EMI -2-(3-methylpyridyl) —CH₃ —CH₃ EMJ -2-(3-methylpyridyl) —H —H EMK-2-(3-methylpyridyl) —H —Cl EML -2-(3-methylpyridyl) —H —Br EMM-2-(3-methylpyridyl) —H —F EMN -2-(3-methylpyridyl) —H —CH₃ EMO-2-(3-methylpyridyl) —H —CF₃ EMP -2-(3-methylpyridyl) —H —OCH₃ EMQ-2-(3-methylpyridyl) —H —OCH₂CH₃ EMR -2-(3-methylpyridyl) —H —OCF₃ EMS-2-(3-methylpyridyl) —H -tert-butyl EMT -2-(3-methylpyridyl) —H-iso-propyl EMU -2-(3—CF₃-pyridyl) —Cl —H EMV -2-(3—CF₃-pyridyl) —Br —HEMW -2-(3—CF₃-pyridyl) —F —H EMX -2-(3—CF₃-pyridyl) —CH₃ —H EMY-2-(3—CF₃-pyridyl) —CF₃ —H EMZ -2-(3—CF₃-pyridyl) —OCH₃ —H ENA-2-(3—CF₃-pyridyl) —OCH₂CH₃ —H ENB -2-(3—CF₃-pyridyl) —OCF₃ —H ENC-2-(3—CF₃-pyridyl) -tert-butyl —H END -2-(3—CF₃-pyridyl) -iso-propyl —HENE -2-(3—CF₃-pyridyl) —CH₃ —CH₃ ENF -2-(3—CF₃-pyridyl) —H —H ENG-2-(3—CF₃-pyridyl) —H —Cl ENH -2-(3—CF₃-pyridyl) —H —Br ENI-2-(3—CF₃-pyridyl) —H —F ENJ -2-(3—CF₃-pyridyl) —H —CH₃ ENK-2-(3—CF₃-pyridyl) —H —CF₃ ENL -2-(3—CF₃-pyridyl) —H —OCH₃ ENM-2-(3—CF₃-pyridyl) —H —OCH₂CH₃ ENN -2-(3—CF₃-pyridyl) —H —OCF₃ ENO-2-(3—CF₃-pyridyl) —H -tert-butyl ENP -2-(3—CF₃-pyridyl) —H -zso-propylENQ -4-(5-chloropyrimidinyl) —Cl —H ENR -4-(5-chloropyrimidinyl) —Br —HENS -4-(5-chloropyrimidinyl) —F —H ENT -4-(5-chloropyrimidinyl) —CH₃ —HENU -4-(5-chloropyrimidinyl) —CF₃ —H ENV -4-(5-chloropyrimidinyl) —OCH₃—H ENW -4-(5-chloropyrimidinyl) —OCH₂CH₃ —H ENX -4-(5-chloropyrimidinyl)—OCF₃—H ENY -4-(5-chloropyrimidinyl) -tert-butyl —H ENZ-4-(5-chloropyrimidinyl) -iso-propyl —H EOA -4-(5-chloropyrimidinyl)—CH₃ —CH₃ EOB -4-(5-chloropyrimidinyl) —H —H EOC-4-(5-chloropyrimidinyl) —H —Cl EOD -4-(5-chloropyrimidinyl) —H —Br EOE-4-(5-chloropyrimidinyl) —H —F EOF -4-(5-chloropyrimidinyl) —H —CH₃ EOG-4-(5-chloropyrimidinyl) —H —CF₃ EOH -4-(5-chloropyrimidinyl) —H —OCH₃EOI -4-(5-chloropyrimidinyl) —H —OCH₂CH₃ EOJ -4-(5-chloropyrimidinyl) —H—OCF₃ EOK -4-(5-chloropyrimidinyl) —H -tert-butyl EOL-4-(5-chloropyrimidinyl) —H -iso-propyl EOM -4-(5-methylpyrimidinyl) —Cl—H EON -4-(5-methylpyrimidinyl) —Br —H EOO -4-(5-methylpyrimidinyl) —F—H EOP -4-(5-methylpyrimidinyl) —CH₃ —H EOQ -4-(5-methylpyrimidinyl)—CF₃ —H EOR -4-(5-methylpyrimidinyl) —OCH₃ —H EOS-4-(5-methylpyrimidinyl) —OCH₂CH₃ —H EOT -4-(5-methylpyrimidinyl) —OCF₃—H EOU -4-(5-methylpyrimidinyl) -tert-butyl —H EOV-4-(5-methylpyrimidinyl) -iso-propyl —H EOW -4-(5-methylpyrimidinyl)—CH₃ —CH₃ EOX -4-(5-methylpyrimidinyl) —H —H EOY-4-(5-methylpyrimidinyl) —H —Cl EOZ -4-(5-methylpyrimidinyl) —H —Br EPA-4-(5-methylpyrimidinyl) —H —F EPB -4-(5-methylpyrimidinyl) —H —CH₃ EPC-4-(5-methylpyrimidinyl) —H —CF₃ EPD -4-(5-methylpyrimidinyl) —H —OCH₃EPE -4-(5-methylpyrimidinyl) —H —OCH₂CH₃ EPF -4-(5-methylpyrimidinyl) —H—OCF₃ EPG -4-(5-methylpyrimidinyl) —H -tert-butyl EPH-4-(5-methylpyrimidinyl) —H -iso-propyl EPI -2-pyrazinyl —Cl —H EPJ-2-pyrazinyl —Br —H EPK -2-pyrazinyl —F —H EPL -2-pyrazinyl —CH₃ —H EPM-2-pyrazinyl —CF₃ —H EPN -2-pyrazinyl —OCH₃ —H EPO -2-pyrazinyl —OCH₂CH₃—H EPP -2-pyrazinyl —OCF₃ —H EPQ -2-pyrazinyl -tert-butyl —H EPR-2-pyrazinyl -iso-propyl —H EPS -2-pyrazinyl —CH₃ —CH₃ EPT -2-pyrazrnyl—H —H EPU -2-pyrazinyl —H —Cl EPV -2-pyrazinyl —H —Br EPW -2-pyrazinyl—H —F EPX -2-pyrazinyl —H —CH₃ EPY -2-pyrazinyl —H —CF₃ EPZ -2-pyrazinyl—H —OCH₃ EQA -2-pyrazinyl —H —OCH₂CH₃ EQB -2-pyrazinyl —H —OCF₃ EQC-2-pyrazinyl —H -tert-butyl EQD -2-pyrazinyl —H -iso-propyl EQE-2-(3-chloropyrazinyl) —Cl —H EQF -2-(3-chloropyrazinyl) —Br —H EQG-2-(3-chloropyrazinyl) —F —H EQH -2-(3-chloropyrazinyl) —CH₃ —H EQI-2-(3-chloropyrazinyl) —CF₃ —H EQJ -2-(3-chloropyrazinyl) —OCH₃ —H EQK-2-(3-chloropyrazinyl) —OCH₂CH₃ —H EQL -2-(3-chloropyrazinyl) —OCF₃ —HEQM -2-(3-chloropyrazinyl) -tert-butyl —H EQN -2-(3-chloropyrazinyl)-iso-propyl —H EQO -2-(3-chloropyrazinyl) —CH₃ —CH₃ EQP-2-(3-chloropyrazinyl) —H —H EQQ -2-(3-chloropyrazinyl) —H —Cl EQR-2-(3-chloropyrazinyl) —H —Br EQS -2-(3-chloropyrazinyl) —H —F EQT-2-(3-chloropyrazinyl) —H —CH₃ EQU -2-(3-chloropyrazinyl) —H —CF₃ EQV-2-(3-chloropyrazinyl) —H —OCH₃ EQW -2-(3-chloropyrazinyl) —H —OCH₂CH₃EQX -2-(3-chloropyrazinyl) —H —OCF₃ EQY -2-(3-chloropyrazinyl) —H-tert-butyl EQZ -2-(3-chloropyrazinyl) —H -iso-propyl ERA-2-(3-methylpyrazinyl) —Cl —H ERB -2-(3-methylpyrazinyl) —Br —H ERC-2-(3-methylpyrazinyl) —F —H ERD -2-(3-methylpyrazinyl) —CH₃ —H ERE-2-(3-methylpyrazinyl) —CF₃ —H ERF -2-(3-methylpyrazinyl) —OCH₃ —H ERG-2-(3-methylpyrazinyl) —OCH₂CH₃ —H ERH -2-(3-methylpyrazinyl) —OCF₃ —HERI -2-(3-methylpyrazinyl) -tert-butyl —H ERJ -2-(3-methylpyrazinyl)-iso-propyl —H ERK -2-(3-methylpyrazinyl) —CH₃ —CH₃ ERL-2-(3-methylpyrazinyl) —H —H ERM -2-(3-methylpyrazinyl) —H —Cl ERN-2-(3-methylpyrazinyl) —H —Br ERO -2-(3-methylpyrazinyl) —H —F ERP-2-(3-methylpyrazinyl) —H —CH₃ ERQ -2-(3-methylpyrazinyl) —H —CF₃ ERR-2-(3-methylpyrazinyl) —H —OCH₃ ERS -2-(3-methylpyrazinyl) —H —OCH₂CH₃ERT -2-(3-methylpyrazinyl) —H —OCF₃ ERU -2-(3-methylpyrazinyl) —H-tert-butyl ERV -2-(3-methylpyrazinyl) —H -iso-propyl ERW -2-pyridazinyl—Cl —H ERX -2-pyridazinyl —Br —H ERY -2-pyridazinyl —F —H ERZ-2-pyridazinyl —CH₃ —H ESA -2-pyridazinyl —CF₃ —H ESB -2-pyridazinyl—OCH₃ —H ESC -2-pyridazinyl —OCH₂CH₃ —H ESD -2-pyridazinyl —OCF₃ —H ESE-2-pyridazinyl -tert-butyl —H ESF -2-pyridazinyl -iso-propyl —H ESG-2-pyridazinyl —CH₃ —CH₃ ESH -2-pyridazinyl —H —H ESI -2-pyridazinyl —H—Cl ESJ -2-pyridazinyl —H —Br ESK -2-pyridazinyl —H —F ESL-2-pyridazinyl —H —CH₃ ESM -2-pyridazinyl —H —CF₃ ESN -2-pyridazinyl —H—OCH₃ ESO -2-pyridazinyl —H —OCH₂CH₃ ESP -2-pyridazinyl —H —OCF₃ ESQ-2-pyridazinyl —H -tert-butyl ESR -2-pyridazinyl —H -iso-propyl ESS-3-(4-chloropyridazinyl) —Cl —H EST -3-(4-chloropyridazinyl) —Br —H ESU-3-(4-chloropyridazinyl) —F —H ESV -3-(4-chloropyridazinyl) —CH₃ —H ESW-3-(4-chloropyridazinyl) —CF₃ —H ESX -3-(4-chloropyridazinyl)—OCH_(3 —H) ESY -3-(4-chloropyridazinyl) —OCH₂CH₃ —H ESZ-3-(4-chloropyridazinyl) —OCF_(3 —H) ETA -3-(4-chloropyridazinyl)-tert-butyl —H ETB -3-(4-chloropyridazinyl) -zso-propyl —H ETC-3-(4-chloropyridazinyl) —CH₃ —CH₃ ETD -3-(4-chloropyridazinyl) —H —HETE -3-(4-chloropyridazinyl) —H —Cl ETF -3-(4-chloropyridazinyl) —H —BrETG -3-(4-chloropyridazinyl) —H —F ETH -3-(4-chloropyridazinyl) —H —CH₃ETI -3-(4-chloropyridazinyl) —H —CF₃ ETJ -3-(4-chloropyridazinyl) —H—OCH₃ ETK -3-(4-chloropyridazinyl) —H —OCH₂CH₃ ETL-3-(4-chloropyridazinyl) —H —OCF₃ ETM -3-(4-chloropyridazinyl) —H-tert-butyl ETN -3-(4-chloropyridazinyl) —H -iso-propyl ETO-3-(4-methylpyridazinyl) —Cl —H ETP -3-(4-methylpyridazinyl) —Br —H ETQ-3-(4-methylpyridazinyl) —F —H ETR -3-(4-methylpyridazinyl) —CH₃ —H ETS-3-(4-methylpyridazinyl) —CF₃ —H ETT -3-(4-methylpyridazinyl) —OCH₃ —HETU -3-(4-methylpyridazinyl) —OCH₂CH₃ —H ETV -3-(4-methylpyridazinyl)—OCF₃ —H ETW -3-(4-methylpyridazinyl) -tert-butyl —H ETX-3-(4-methylpyridazinyl) -iso-propyl —H ETY -3-(4-methylpyridazinyl)—CH₃ —CH₃ ETZ -3-(4-methylpyridazinyl) —H —H EUA-3-(4-methylpyridazinyl) —H —Cl EUB -3-(4-methylpyridazinyl) —H —Br EUC-3-(4-methylpyridazinyl) —H —F EUD -3-(4-methylpyridazinyl) —H —CH₃ EUE-3-(4-methylpyridazinyl) —H —CF₃ EUF -3-(4-methylpyridazinyl) —H —OCH₃EUG -3-(4-methylpyridazinyl) —H —OCH₂CH₃ EUH -3-(4-methylpyridazinyl) —H—OCF₃ EUI -3-(4-methylpyridazinyl) —H -tert-butyl EUJ-3-(4-methylpyridazinyl) —H -iso-propyl EUK -4-thiazanyl —Cl —H EUL-4-thiazanyl —Br —H EUM -4-thiazanyl —F —H EUN -4-thiazanyl —CH₃ —H EUO-4-thiazanyl —CF₃ —H EUP -4-thiazanyl —OCH₃ —H EUQ -4-thiazanyl —OCH₂CH₃—H EUR -4-thiazanyl —OCF₃ —H EUS -4-thiazanyl -tert-butyl —H EUT-4-thiazanyl -iso-propyl —H EUU -4-thiazanyl —CH₃ —CH₃ EUV -4-thiazanyl—H —H EUW -4-thiazanyl —H —Cl EUX -4-thiazanyl —H —Br EUY -4-thiazanyl—H —F EUZ -4-thiazanyl —H —CH₃ EVA -4-thiazanyl —H —CF₃ EVB -4-thiazanyl—H —OCH₃ EVC -4-thiazanyl —H —OCH₂CH₃ EVD -4-thiazanyl —H —OCF₃ EVE-4-thiazanyl —H -tert-butyl EVF -4-thiazanyl —H -iso-propyl EVG-5-(4-chlorothiazanyl) —Cl —H EVH -5-(4-chlorothiazanyl) —Br —H EVI-5-(4-chlorothiazanyl) —F —H EVJ -5-(4-chlorothiazanyl) —CH₃ —H EVK-5-(4-chlorothiazanyl) —CF₃ —H EVL -5-(4-chlorothiazanyl) —OCH₃ —H EVM-5-(4-chlorothiazanyl) —OCH₂CH₃ —H EVN -5-(4-chlorothiazanyl) —OCF₃ —HEVO -5-(4-chlorothiazanyl) -tert-butyl —H EVP -5-(4-chlorothiazanyl)-iso-propyl —H EVQ -5-(4-chlorothiazanyl) —CH₃ —CH₃ EVR-5-(4-chlorothiazanyl) —H —H EVS -5-(4-chlorothiazanyl) —H —Cl EVT-5-(4-chlorothiazanyl) —H —Br EVU -5-(4-chlorothiazanyl) —H —F EVV-5-(4-chlorothiazanyl) —H —CH₃ EVW -5-(4-chlorothiazanyl) —H —CF₃ EVX-5-(4-chlorothiazanyl) —H —OCH₃ EVY -5-(4-chlorothiazanyl) —H —OCH₂CH₃EVZ -5-(4-chlorothiazanyl) —H —OCF₃ EWA -5-(4-chlorothiazanyl) —H-tert-butyl EWB -5-(4-chlorothiazanyl) —H -zso-propyl EWC-5-(4-methylthiazanyl) —Cl —H EWD -5-(4-methylthiazanyl) —Br —H EWE-5-(4-methylthiazanyl) —F —H EWF -5-(4-methylthiazanyl) —CH₃ —H EWG-5-(4-methylthiazanyl) —CF₃ —H EWH -5-(4-methylthiazanyl) —OCH₃ —H EWI-5-(4-methylthiazanyl) —OCH₂CH₃ —H EWJ -5-(4-methylthiazanyl) —OCF₃ —HEWK -5-(4-methylthiazanyl) -tert-butyl —H EWL -5-(4-methylthiazanyl)-iso-propyl —H EWM -5-(4-methylthiazanyl) —CH₃ —CH₃ EWN-5-(4-methylthiazanyl) —H —H EWO -5-(4-methylthiazanyl) —H —Cl EWP-5-(4-methylthiazanyl) —H —Br EWQ -5-(4-methylthiazanyl) —H —F EWR-5-(4-methylthiazanyl) —H —CH₃ EWS -5-(4-methylthiazanyl) —H —CF₃ EWT-5-(4-methylthiazanyl) —H —OCH₃ EWU -5-(4-methylthiazanyl) —H —OCH₂CH₃EWV -5-(4-methylthiazanyl) —H —OCF₃ EWW -5-(4-methylthiazanyl) —H-tert-butyl EWX -5-(4-methylthiazanyl) —H -iso-propyl

TABLE XIV

and pharmaceutically acceptable salts thereof, wherein: Compound Ar₁ R₈R₉ EWY -2-(3-chloropyridyl) —Cl —H EWZ -2-(3-chloropyridyl) —Br —H EXA-2-(3-chloropyridyl) —F —H EXB -2-(3-chloropyridyl) —CH₃ —H EXC-2-(3-chloropyridyl) —CF₃ —H EXD -2-(3-chloropyridyl) —OCH₃ —H EXE-2-(3-chloropyridyl) —OCH₂CH₃ —H EXF -2-(3-chloropyridyl) —OCF₃ —H EXG-2-(3-chloropyridyl) -tert-butyl —H EXH -2-(3-chloropyridyl) -iso-propyl—H EXI -2-(3-chloropyridyl) —CH₃ —CH₃ EXJ -2-(3-chloropyridyl) —H —H EXK-2-(3-chloropyridyl) —H —Cl EXL -2-(3-chloropyridyl) —H —Br EXM-2-(3-chloropyridyl) —H —F EXN -2-(3-chloropyridyl) —H —CH₃ EXO-2-(3-chloropyridyl) —H —CF₃ EXP -2-(3-chloropyridyl) —H —OCH₃ EXQ-2-(3-chloropyridyl) —H —OCH₂CH₃ EXR -2-(3-chloropyridyl) —H —OCF₃ EXS-2-(3-chloropyridyl) —H -tert-butyl EXT -2-(3-chloropyridyl) —H-iso-propyl EXU -2-(3-methylpyridyl) —Cl —H EXV -2-(3-methylpyridyl) —Br—H EXW -2-(3-methylpyridyl) —F —H EXX -2-(3-methylpyridyl) —CH₃ —H EXY-2-(3-methylpyridyl) —CF₃ —H EXZ -2-(3-methylpyridyl) —OCH₃ —H EYA-2-(3-methylpyridyl) —OCH₂CH₃ —H EYB -2-(3-methylpyridyl) —OCF₃ —H EYC-2-(3-methylpyridyl) -tert-butyl —H EYD -2-(3-methylpyridyl) -iso-propyl—H EYE -2-(3-methylpyridyl) —CH₃ —CH₃ EXF -2-(3-methylpyridyl) —H —H EYG-2-(3-methylpyridyl) —H —Cl EYH -2-(3-methylpyridyl) —H —Br EYI-2-(3-methylpyridyl) —H —F EYJ -2-(3-methylpyridyl) —H —CH₃ EYK-2-(3-methylpyridyl) —H —CF₃ EYL -2-(3-methylpyridyl) —H —OCH₃ EYM-2-(3-methylpyridyl) —H —OCH₂CH₃ EYN -2-(3-methylpyridyl) —H —OCF₃ EYO-2-(3-methylpyridyl) —H -tert-butyl EYP -2-(3-methylpyridyl) —H-iso-propyl EYQ -2-(3-CF₃-pyridyl) —Cl —H EYR -2-(3-CF₃-pyridyl) —Br —HEYS -2-(3-CF₃-pyridyl) —F —H EYT -2-(3-CF₃-pyridyl) —CH₃ —H EYU-2-(3-CF₃-pyridyl) —CF₃ —H EYV -2-(3-CF₃-pyridyl) —OCH₃ —H EYW-2-(3-CF₃-pyridyl) —OCH₂CH₃ —H EYX -2-(3-CF₃-pyridyl) —OCF₃ —H EYY-2-(3-CF₃-pyridyl) -tert-butyl —H EYZ -2-(3-CF₃-pyridyl) -iso-propyl —HEZA -2-(3-CF₃-pyridyl) —CH₃ —CH₃ EZB -2-(3-CF₃-pyridyl) —H —H EZC-2-(3-CF₃-pyridyl) —H —Cl EZD -2-(3-CF₃-pyridyl) —H —Br EZE-2-(3-CF₃-pyridyl) —H —F EZF -2-(3-CF₃-pyridyl) —H —CH₃ EZG-2-(3-CF₃-pyridyl) —H —CF₃ EZH -2-(3-CF₃-pyridyl) —H —OCH₃ EZI-2-(3-CF₃-pyridyl) —H —OCH₂CH₃ EZJ -2-(3-CF₃-pyridyl) —H —OCF₃ EZK-2-(3-CF₃-pyridyl) —H -tert-butyl EZL -2-(3-CF₃-pyridyl) —H -iso-propylEZM -4-(5-chloropyrimidinyl) —Cl —H EZN -4-(5-chloropyrimidinyl) —Br —HEZO -4-(5-chloropyrimidinyl) —F —H EZP -4-(5-chloropyrimidinyl) —CH₃ —HEZQ -4-(5-chloropyrimidinyl) —CF₃ —H EZR -4-(5-chloropyrimidinyl) —OCH₃—H EZS -4-(5-chloropyrimidinyl) —OCH₂CH₃ —H EZT -4-(5-chloropyrimidinyl)—OCF₃ —H EZU -4-(5-chloropyrimidinyl) -tert-butyl —H EZV-4-(5-chloropyrimidinyl) -iso-propyl —H EZW -4-(5-chloropyrimidinyl)—CH₃ —CH₃ EZX -4-(5-chloropyrimidinyl) —H —H EZY-4-(5-chloropyrimidinyl) —H —Cl EZZ -4-(5-chloropyrimidinyl) —H —Br FAA-4-(5-chloropyrimidinyl) —H —F FAB -4-(5-chloropyrimidinyl) —H —CH₃ FAC-4-(5-chloropyrimidinyl) —H —CF₃ FAD -4-(5-chloropyrimidinyl) —H —OCH₃FAE -4-(5-chloropyrimidinyl) —H —OCH₂CH₃ FAF -4-(5-chloropyrimidinyl) —H—OCF₃ FAG -4-(5-chloropyrimidinyl) —H -tert-butyl FAH-4-(5-chloropyrimidinyl) —H -iso-propyl FAI -4-(5-methylpyrimidinyl) —Cl—H FAJ -4-(5-methylpyrimidinyl) —Br —H FAK -4-(5-methylpyrimidinyl) —F—H FAL -4-(5-methylpyrimidinyl) —CH₃ —H FAM -4-(5-methylpyrimidinyl)—CF₃ —H FAN -4-(5-methylpyrimidinyl) —OCH₃ —H FAO-4-(5-methylpyrimidinyl) —OCH₂CH₃ —H FAP -4-(5-methylpyrimidinyl) —OCF₃—H FAQ -4-(5-methylpyrimidinyl) -tert-butyl —H FAR-4-(5-methylpyrimidinyl) -iso-propyl —H FAS -4-(5-methylpyrimidinyl)—CH₃ —CH₃ FAT -4-(5-methylpyrimidinyl) —H —H FAU-4-(5-methylpyrimidinyl) —H —Cl FAV -4-(5-methylpyrimidinyl) —H —Br FAW-4-(5-methylpyrimidinyl) —H —F FAX -4-(5-methylpyrimidinyl) —H —CH₃ FAY-4-(5-methylpyrimidinyl) —H —CF₃ FAZ -4-(5-methylpyrimidinyl) —H —OCH₃FBA -4-(5-methylpyrimidinyl) —H —OCH₂CH₃ FBB -4-(5-methylpyrimidinyl) —H—OCF₃ FBC -4-(5-methylpyrimidinyl) —H -tert-butyl FBD-4-(5-methylpyrimidinyl) —H -iso-propyl FBE -2-pyrazinyl —Cl —H FBF-2-pyrazinyl —Br —H FBG -2-pyrazinyl —F —H FBH -2-pyrazinyl —CH₃ —H FBI-2-pyrazinyl —CF₃ —H FBJ -2-pyrazinyl —OCH₃ —H FBK -2-pyrazinyl —OCH₂CH₃—H FBL -2-pyrazinyl —OCF₃ —H FBM -2-pyrazinyl -tert-butyl —H FBN-2-pyrazinyl -iso-propyl —H FBO -2-pyrazinyl —CH₃ —CH₃ FBP -2-pyrazinyl—H —H FBQ -2-pyrazinyl —H —Cl FBR -2-pyrazinyl —H —Br FBS -2-pyrazinyl—H —F FBT -2-pyrazinyl —H —CH₃ FBU -2-pyrazinyl —H —CF₃ FBV -2-pyrazinyl—H —OCH₃ FBW -2-pyrazinyl —H —OCH₂CH₃ FBX -2-pyrazinyl —H —OCF₃ FBY-2-pyrazinyl —H -tert-butyl FBZ -2-pyrazinyl —H -iso-propyl FCA-2-(3-chloropyrazinyl) —Cl —H FCB -2-(3-chloropyrazinyl) —Br —H FCC-2-(3-chloropyrazinyl) —F —H FCD -2-(3-chloropyrazinyl) —CH₃ —H FCE-2-(3-chloropyrazinyl) —CF₃ —H FCF -2-(3-chloropyrazinyl) —OCH₃ —H FCG-2-(3-chloropyrazinyl) —OCH₂CH₃ —H FCH -2-(3-chloropyrazinyl) —OCF₃ —HFCI -2-(3-chloropyrazinyl) -tert-butyl —H FCJ -2-(3-chloropyrazinyl)-iso-propyl —H FCK -2-(3-chloropyrazinyl) —CH₃ —CH₃ FCL-2-(3-chloropyrazinyl) —H —H FCM -2-(3-chloropyrazinyl) —H —Cl FCN-2-(3-chloropyrazinyl) —H —Br FCO -2-(3-chloropyrazinyl) —H —F FCP-2-(3-chloropyrazinyl) —H —CH₃ FCQ -2-(3-chloropyrazinyl) —H —CF₃ FCR-2-(3-chloropyrazinyl) —H —OCH₃ FCS -2-(3-chloropyrazinyl) —H —OCH₂CH₃FCT -2-(3-chloropyrazinyl) —H —OCF₃ FCU -2-(3-chloropyrazinyl) —H-tert-butyl FCV -2-(3-chloropyrazinyl) —H -iso-propyl FCW-2-(3-methylpyrazinyl) —Cl —H FCX -2-(3-methylpyrazinyl) —Br —H FCY-2-(3-methylpyrazinyl) —F —H FCZ -2-(3-methylpyrazinyl) —CH₃ —H FDA-2-(3-methylpyrazinyl) —CF₃ —H FDB -2-(3-methylpyrazinyl) —OCH₃ —H FDC-2-(3-methylpyrazinyl) —OCH₂CH₃ —H FDD -2-(3-methylpyrazinyl) —OCF₃ —HFDE -2-(3-methylpyrazinyl) -tert-butyl —H FDF -2-(3-methylpyrazinyl)-iso-propyl —H FDG -2-(3-methylpyrazinyl) —CH₃ —CH₃ FDH-2-(3-methylpyrazinyl) —H —H FDI -2-(3-methylpyrazinyl) —H —Cl FDJ-2-(3-methylpyrazinyl) —H —Br FDK -2-(3-methylpyrazinyl) —H —F FDL-2-(3-methylpyrazinyl) —H —CH₃ FDM -2-(3-methylpyrazinyl) —H —CF₃ FDN-2-(3-methylpyrazinyl) —H —OCH₃ FDO -2-(3-methylpyrazinyl) —H —OCH₂CH₃FDP -2-(3-methylpyrazinyl) —H —OCF₃ FDQ -2-(3-methylpyrazinyl) —H-tert-butyl FDR -2-(3-methylpyrazinyl) —H -iso-propyl FDS -2-pyridazinyl—Cl —H FDT -2-pyridazinyl —Br —H FDU -2-pyridazinyl —F —H FDV-2-pyridazinyl —CH₃ —H FDW -2-pyridazinyl —CF₃ —H FDX -2-pyridazinyl—OCH₃ —H FDY -2-pyridazinyl —OCH₂CH₃ —H FDZ -2-pyridazinyl —OCF₃ —H FEA-2-pyridazinyl -tert-butyl —H FEB -2-pyridazinyl -iso-propyl —H FEC-2-pyridazinyl —CH₃ —CH₃ FED -2-pyridazinyl —H —H FEE -2-pyridazinyl —H—Cl FEF -2-pyridazinyl —H —Br FEG -2-pyridazinyl —H —F FEH-2-pyridazinyl —H —CH₃ FEI -2-pyridazinyl —H —CF₃ FEJ -2-pyridazinyl —H—OCH₃ FEK -2-pyridazinyl —H —OCH₂CH₃ FEL -2-pyridazinyl —H —OCF₃ FEM-2-pyridazinyl —H -tert-butyl FEN -2-pyridazinyl —H -iso-propyl FEO-3-(4-chloropyridazinyl) —Cl —H FEP -3-(4-chloropyridazinyl) —Br —H FEQ-3-(4-chloropyridazinyl) —F —H FER -3-(4-chloropyridazinyl) —CH₃ —H FES-3-(4-chloropyridazinyl) —CF₃ —H FET -3-(4-chloropyridazinyl) —OCH₃ —HFEU -3-(4-chloropyridazinyl) —OCH₂CH₃ —H FEV -3-(4-chloropyridazinyl)—OCF₃ —H FEW -3-(4-chloropyridazinyl) -tert-butyl —H FEX-3-(4-chloropyridazinyl) -iso-propyl —H FEY -3-(4-chloropyridazinyl)—CH₃ —CH₃ FEZ -3-(4-chloropyridazinyl) —H —H FFA-3-(4-chloropyridazinyl) —H —Cl FFB -3-(4-chloropyridazinyl) —H —Br FFC-3-(4-chloropyridazinyl) —H —F FFD -3-(4-chloropyridazinyl) —H —CH₃ FFE-3-(4-chloropyridazinyl) —H —CF₃ FFF -3-(4-chloropyridazinyl) —H —OCH₃FFG -3-(4-chloropyridazinyl) —H —OCH₂CH₃ FFH -3-(4-chloropyridazinyl) —H—OCF₃ FFI -3-(4-chloropyridazinyl) —H -tert-butyl FFJ-3-(4-chloropyridazinyl) —H -iso-propyl FFK -3-(4-methylpyridazinyl) —Cl—H FFL -3-(4-methylpyridazinyl) —Br —H FFM -3-(4-methylpyridazinyl) —F—H FFN -3-(4-methylpyridazinyl) —CH₃ —H FFO -3-(4-methylpyridazinyl)—CF₃ —H FFP -3-(4-methylpyridazinyl) —OCH₃ —H FFQ-3-(4-methylpyridazinyl) —OCH₂CH₃ —H FFR -3-(4-methylpyridazinyl) —OCF₃—H FFS -3-(4-methylpyridazinyl) -tert-butyl —H FFT-3-(4-methylpyridazinyl) -iso-propyl —H FFU -3-(4-methylpyridazinyl)—CH₃ —CH₃ FFV -3-(4-methylpyridazinyl) —H —H FFW-3-(4-methylpyridazinyl) —H —Cl FFX -3-(4-methylpyridazinyl) —H —Br FFY-3-(4-methylpyridazinyl) —H —F FFZ -3-(4-methylpyridazinyl) —H —CH₃ FGA-3-(4-methylpyridazinyl) —H —CF₃ FGB -3-(4-methylpyridazinyl) —H —OCH₃FGC -3-(4-methylpyridazinyl) —H —OCH₂CH₃ FGD -3-(4-methylpyridazinyl) —H—OCF₃ FGE -3-(4-methylpyridazinyl) —H -tert-butyl FGF-3-(4-methylpyridazinyl) —H -iso-propyl FGG -4-thiazanyl —Cl —H FGH-4-thiazanyl —Br —H FGI -4-thiazanyl —F —H FGJ -4-thiazanyl —CH₃ —H FGK-4-thiazanyl —CF₃ —H FGL -4-thiazanyl —OCH₃ —H FGM -4-thiazanyl —OCH₂CH₃—H FGN -4-thiazanyl —OCF₃ —H FGO -4-thiazanyl -tert-butyl —H FGP-4-thiazanyl -iso-propyl —H FGQ -4-thiazanyl —CH₃ —CH₃ FGR -4-thiazanyl—H —H FGS -4-thiazanyl —H —Cl FGT -4-thiazanyl —H —Br FGU -4-thiazanyl—H —F FGV -4-thiazanyl —H —CH₃ FGW -4-thiazanyl —H —CF₃ FGX -4-thiazanyl—H —OCH₃ FGY -4-thiazanyl —H —OCH₂CH₃ FGZ -4-thiazanyl —H —OCF₃ FHA-4-thiazanyl —H -tert-butyl FHB -4-thiazanyl —H -iso-propyl FHC-5-(4-chlorothiazanyl) —Cl —H FHD -5-(4-chlorothiazanyl) —Br —H FHE-5-(4-chlorothiazanyl) —F —H FHF -5-(4-chlorothiazanyl) —CH₃ —H FHG-5-(4-chlorothiazanyl) —CF₃ —H FHH -5-(4-chlorothiazanyl) —OCH₃ —H FHI-5-(4-chlorothiazanyl) —OCH₂CH₃ —H FHJ -5-(4-chlorothiazanyl) —OCF₃ —HFHK -5-(4-chlorothiazanyl) -tert-butyl —H FHL -5-(4-chlorothiazanyl)-iso-propyl —H FHM -5-(4-chlorothiazanyl) —CH₃ —CH₃ FHN-5-(4-chlorothiazanyl) —H —H FHO -5-(4-chlorothiazanyl) —H —Cl FHP-5-(4-chlorothiazanyl) —H —Br FHQ -5-(4-chlorothiazanyl) —H —F FHR-5-(4-chlorothiazanyl) —H —CH₃ FHS -5-(4-chlorothiazanyl) —H —CF₃ FHT-5-(4-chlorothiazanyl) —H —OCH₃ FHU -5-(4-chlorothiazanyl) —H —OCH₂CH₃FHV -5-(4-chlorothiazanyl) —H —OCF₃ FHW -5-(4-chlorothiazanyl) —H-tert-butyl FHX -5-(4-chlorothiazanyl) —H -iso-propyl FHY-5-(4-methylthiazanyl) —Cl —H FHZ -5-(4-methylthiazanyl) —Br —H FIA-5-(4-methylthiazanyl) —F —H FIB -5-(4-methylthiazanyl) —CH₃ —H FIC-5-(4-methylthiazanyl) —CF₃ —H FID -5-(4-methylthiazanyl) —OCH₃ —H FIE-5-(4-methylthiazanyl) —OCH₂CH₃ —H FIF -5-(4-methylthiazanyl) —OCF₃ —HFIG -5-(4-methylthiazanyl) -tert-butyl —H FIH -5-(4-methylthiazanyl)-iso-propyl —H FII -5-(4-methylthiazanyl) —CH₃ —CH₃ FIJ-5-(4-methylthiazanyl) —H —H FIK -5-(4-methylthiazanyl) —H —Cl FIL-5-(4-methylthiazanyl) —H —Br FIM -5-(4-methylthiazanyl) —H —F FIN-5-(4-methylthiazanyl) —H —CH₃ FIO -5-(4-methylthiazanyl) —H —CF₃ FIP-5-(4-methylthiazanyl) —H —OCH₃ FIQ -5-(4-methylthiazanyl) —H —OCH₂CH₃FIR -5-(4-methylthiazanyl) —H —OCF₃ FIS -5-(4-methylthiazanyl) —H-tert-butyl FIT -5-(4-methylthiazanyl) —H -iso-propyl

TABLE XV

and pharmaceutically acceptable salts thereof, wherein: Compound Ar₁ R₈R₉ FIU (a, b, and c) -2-(3-chloropyridyl) —Cl —H FIV (a, b, and c)-2-(3-chloropyridyl) —Br —H FIW (a, b, and c) -2-(3-chloropyridyl) —F —HFIX (a, b, and c) -2-(3-chloropyridyl) —CH₃ —H FLY (a, b, and c)-2-(3-chloropyridyl) —CF₃ —H FIZ (a, b, and c) -2-(3-chloropyridyl)—OCH₃ —H FJA (a, b, and c) -2-(3-chloropyridyl) —OCH₂CH₃ —H FJB (a, b,and c) -2-(3-chloropyridyl) —OCF₃ —H FJC (a, b, and c)-2-(3-chloropyridyl) -tert-butyl —H FJD (a, b, and c)-2-(3-chloropyridyl) -iso-propyl —H FJE (a, b, and c)-2-(3-chloropyridyl) —CH₃ —CH₃ FJF (a, b, and c) -2-(3-chloropyridyl) —H—H FJG (a, b, and c) -2-(3-chloropyridyl) —H —Cl FJH (a, b, and c)-2-(3-chloropyridyl) —H —Br FJI (a, b, and c) -2-(3-chloropyridyl) —H —FFJJ (a, b, and c) -2-(3-chloropyridyl) —H —CH₃ FJK (a, b, and c)-2-(3-chloropyridyl) —H —CF₃ FJL (a, b, and c) -2-(3-chloropyridyl) —H—OCH₃ FJM (a, b, and c) -2-(3-chloropyridyl) —H —OCH₂CH₃ FJN (a, b, andc) -2-(3-chloropyridyl) —H —OCF₃ FJO (a, b, and c) -2-(3-chloropyridyl)—H -tert-butyl FJP (a, b, and c) -2-(3-chloropyridyl) —H -iso-propyl FJQ(a, b, and c) -2-(3-methylpyridyl) —Cl —H FJR (a, b, and c)-2-(3-methylpyridyl) —Br —H FJS (a, b, and c) -2-(3-methylpyridyl) —F —HFJT (a, b, and c) -2-(3-methylpyridyl) —CH₃ —H FJU (a, b, and c)-2-(3-methylpyridyl) —CF₃ —H FJV (a, b, and c) -2-(3-methylpyridyl)—OCH₃ —H FJW (a, b, and c) -2-(3-methylpyridyl) —OCH₂CH₃ —H FJX (a, b,and c) -2-(3-methylpyridyl) —OCF₃ —H FJY (a, b, and c)-2-(3-methylpyridyl) -tert-butyl —H FJZ (a, b, and c)-2-(3-methylpyridyl) -iso-propyl —H FKA (a, b, and c)-2-(3-methylpyridyl) —CH₃ —CH₃ FKB (a, b, and c) -2-(3-methylpyridyl) —H—H FKC (a, b, and c) -2-(3-methylpyridyl) —H —Cl FKD (a, b, and c)-2-(3-methylpyridyl) —H —Br FKE (a, b, and c) -2-(3-methylpyridyl) —H —FFKF (a, b, and c) -2-(3-methylpyridyl) —H —CH₃ FKG (a, b, and c)-2-(3-methylpyridyl) —H —CF₃ FKH (a, b, and c) -2-(3-methylpyridyl) —H—OCH₃ FKI (a, b, and c) -2-(3-methylpyridyl) —H —OCH₂CH₃ FKJ (a, b, andc) -2-(3-methylpyridyl) —H —OCF₃ FKK (a, b, and c) -2-(3-methylpyridyl)—H -tert-butyl FKL (a, b, and c) -2-(3-methylpyridyl) —H -iso-propyl FKM(a, b, and c) -2-(3-CF₃-pyridyl) —Cl —H FKN (a, b, and c)-2-(3-CF₃-pyridyl) —Br —H FKO (a, b, and c) -2-(3-CF₃-pyridyl) —F —H FKP(a, b, and c) -2-(3-CF₃-pyridyl) —CH₃ —H FKQ (a, b, and c)-2-(3-CF₃-pyridyl) —CF₃ —H FKR (a, b, and c) -2-(3-CF₃-pyridyl) —OCH₃ —HFKS (a, b, and c) -2-(3-CF₃-pyridyl) —OCH₂CH₃ —H FKT (a, b, and c)-2-(3-CF₃-pyridyl) —OCF₃ —H FKU (a, b, and c) -2-(3-CF₃-pyridyl)-tert-butyl —H FKV (a, b, and c) -2-(3-CF₃-pyridyl) -iso-propyl —H FKW(a, b, and c) -2-(3-CF₃-pyridyl) —CH₃ —CH₃ FKX (a, b, and c)-2-(3-CF₃-pyridyl) —H —H FKY (a, b, and c) -2-(3-CF₃-pyridyl) —H —Cl FKZ(a, b, and c) -2-(3-CF₃-pyridyl) —H —Br FLA (a, b, and c)-2-(3-CF₃-pyridyl) —H —F FLB (a, b, and c) -2-(3-CF₃-pyridyl) —H —CH₃FLC (a, b, and c) -2-(3-CF₃-pyridyl) —H —CF₃ FLD (a, b, and c)-2-(3-CF₃-pyridyl) —H —OCH₃ FLE (a, b, and c) -2-(3-CF₃-pyridyl) —H—OCH₂CH₃ FLF (a, b, and c) -2-(3-CF₃-pyridyl) —H —OCF₃ FLG (a, b, and c)-2-(3-CF₃-pyridyl) —H -tert-butyl FLH (a, b, and c) -2-(3-CF₃-pyridyl)—H -iso-propyl FLI (a, b, and c) -4-(5-chloropyrimidinyl) —Cl —H FLJ (a,b, and c) -4-(5-chloropyrimidinyl) —Br —H FLK (a, b, and c)-4-(5-chloropyrimidinyl) —F —H FLL (a, b, and c)-4-(5-chloropyrimidinyl) —CH₃ —H FLM (a, b, and c)-4-(5-chloropyrimidinyl) —CF₃ —H FLN (a, b, and c)-4-(5-chloropyrimidinyl) —OCH₃ —H FLO (a, b, and c)-4-(5-chloropyrimidinyl) —OCH₂CH₃ —H FLP (a, b, and c)-4-(5-chloropyrimidinyl) —OCF₃ —H FLQ (a, b, and c)-4-(5-chloropyrimidinyl) -tert-butyl —H FLR (a, b, and c)-4-(5-chloropyrimidinyl) -iso-propyl —H FLS (a, b, and c)-4-(5-chloropyrimidinyl) —CH₃ —CH₃ FLT (a, b, and c)-4-(5-chloropyrimidinyl) —H —H FLU (a, b, and c)-4-(5-chloropyrimidinyl) —H —Cl FLV (a, b, and c)-4-(5-chloropyrimidinyl) —H —Br FLW (a, b, and c)-4-(5-chloropyrimidinyl) —H —F FLX (a, b, and c)-4-(5-chloropyrimidinyl) —H —CH₃ FLY (a, b, and c)-4-(5-chloropyrimidinyl) —H —CF₃ FLZ (a, b, and c)-4-(5-chloropyrimidinyl) —H —OCH₃ FMA (a, b, and c)-4-(5-chloropyrimidinyl) —H —OCH₂CH₃ FMB (a, b, and c)-4-(5-chloropyrimidinyl) —H —OCF₃ FMC (a, b, and c)-4-(5-chloropyrimidinyl) —H -tert-butyl FMD (a, b, and c)-4-(5-chloropyrimidinyl) —H -iso-propyl FME (a, b, and c)-4-(5-methylpyrimidinyl) —Cl —H FMF (a, b, and c)-4-(5-methylpyrimidinyl) —Br —H FMG (a, b, and c)-4-(5-methylpyrimidinyl) —F —H FMH (a, b, and c)-4-(5-methylpyrimidinyl) —CH₃ —H FMI (a, b, and c)-4-(5-methylpyrimidinyl) —CF₃ —H FMJ (a, b, and c)-4-(5-methylpyrimidinyl) —OCH₃ —H FMK (a, b, and c)-4-(5-methylpyrimidinyl) —OCH₂CH₃ —H FML (a, b, and c)-4-(5-methylpyrimidinyl) —OCF₃ —H FMM -4-(5-methylpyrimidinyl)-tert-butyl —H (a, b, and c) FMN (a, b, and c) -4-(5-methylpyrimidinyl)-iso-propyl —H FMO (a, b, and c) -4-(5-methylpyrimidinyl) —CH₃ —CH₃ FMP(a, b, and c) -4-(5-methylpyrimidinyl) —H —H FMQ (a, b, and c)-4-(5-methylpyrimidinyl) —H —Cl FMR (a, b, and c)-4-(5-methylpyrimidinyl) —H —Br FMS (a, b, and c)-4-(5-methylpyrimidinyl) —H —F FMT (a, b, and c)-4-(5-methylpyrimidinyl) —H —CH₃ FMU (a, b, and c)-4-(5-methylpyrimidinyl) —H —CF₃ FMV (a, b, and c)-4-(5-methylpyrimidinyl) —H —OCH₃ FMW -4-(5-methylpyrimidinyl) —H—OCH₂CH₃ (a, b, and c) FMX (a, b, and c) -4-(5-methylpyrimidinyl) —H—OCF₃ FMY (a, b, and c) -4-(5-methylpyrimidinyl) —H -tert-butyl FMZ (a,b, and c) -4-(5-methylpyrimidinyl) —H -iso-propyl FNA (a, b, and c)-2-pyrazinyl —Cl —H FNB (a, b, and c) -2-pyrazinyl —Br —H FNC (a, b, andc) -2-pyrazinyl —F —H FND (a, b, and c) -2-pyrazinyl —CH₃ —H FNE (a, b,and c) -2-pyrazinyl —CF₃ —H FNF (a, b, and c) -2-pyrazinyl —OCH₃ —H FNG(a, b, and c) -2-pyrazinyl —OCH₂CH₃ —H FNH (a, b, and c) -2-pyrazinyl—OCF₃ —H FNI (a, b, and c) -2-pyrazinyl -tert-butyl —H FNJ (a, b, and c)-2-pyrazinyl -iso-propyl —H FNK (a, b, and c) -2-pyrazinyl —CH₃ —CH₃ FNL(a, b, and c) -2-pyrazinyl —H —H FNM (a, b, and c) -2-pyrazinyl —H —ClFNN (a, b, and c) -2-pyrazinyl —H —Br FNO (a, b, and c) -2-pyrazinyl —H—F FNP (a, b, and c) -2-pyrazinyl —H —CH₃ FNQ (a, b, and c) -2-pyrazinyl—H —CF₃ FNR (a, b, and c) -2-pyrazinyl —H —OCH₃ FNS (a, b, and c)-2-pyrazinyl —H —OCH₂CH₃ FNT (a, b, and c) -2-pyrazinyl —H —OCF₃ FNU (a,b, and c) -2-pyrazinyl —H -tert-butyl FNV (a, b, and c) -2-pyrazinyl —H-iso-propyl FNW (a, b, and c) -2-(3-chloropyrazinyl) —Cl —H FNX (a, b,and c) -2-(3-chloropyrazinyl) —Br —H FNY (a, b, and c)-2-(3-chloropyrazinyl) —F —H FNZ (a, b, and c) -2-(3-chloropyrazinyl)—CH₃ —H FOA (a, b, and c) -2-(3-chloropyrazinyl) —CF₃ —H FOB (a, b, andc) -2-(3-chloropyrazinyl) —OCH₃ —H FOC (a, b, and c)-2-(3-chloropyrazinyl) —OCH₂CH₃ —H FOD (a, b, and c)-2-(3-chloropyrazinyl) —OCF₃ —H FOE (a, b, and c) -2-(3-chloropyrazinyl)-tert-butyl —H FOF (a, b, and c) -2-(3-chloropyrazinyl) -iso-propyl —HFOG (a, b, and c) -2-(3-chloropyrazinyl) —CH₃ —CH₃ FOH (a, b, and c)-2-(3-chloropyrazinyl) —H —H FOI (a, b, and c) -2-(3-chloropyrazinyl) —H—Cl FOJ (a, b, and c) -2-(3-chloropyrazinyl) —H —Br FOK (a, b, and c)-2-(3-chloropyrazinyl) —H —F FOL (a, b, and c) -2-(3-chloropyrazinyl) —H—CH₃ FOM (a, b, and c) -2-(3-chloropyrazinyl) —H —CF₃ FON (a, b, and c)-2-(3-chloropyrazinyl) —H —OCH₃ FOO (a, b, and c) -2-(3-chloropyrazinyl)—H —OCH₂CH₃ FOP (a, b, and c) -2-(3-chloropyrazinyl) —H —OCF₃ FOQ (a, b,and c) -2-(3-chloropyrazinyl) —H -tert-butyl FOR (a, b, and c)-2-(3-chloropyrazinyl) —H -iso-propyl FOS (a, b, and c)-2-(3-methylpyrazinyl) —Cl —H FOT (a, b, and c) -2-(3-methylpyrazinyl)—Br —H FOU (a, b, and c) -2-(3-methylpyrazinyl) —F —H FOV (a, b, and c)-2-(3-methylpyrazinyl) —CH₃ —H FOW (a, b, and c) -2-(3-methylpyrazinyl)—CF₃ —H FOX (a, b, and c) -2-(3-methylpyrazinyl) —OCH₃ —H FOY (a, b, andc) -2-(3-methylpyrazinyl) —OCH₂CH₃ —H FOZ (a, b, and c)-2-(3-methylpyrazinyl) —OCF₃ —H FPA (a, b, and c) -2-(3-methylpyrazinyl)-tert-butyl —H FPB (a, b, and c) -2-(3-methylpyrazinyl) -iso-propyl —HFPC (a, b, and c) -2-(3-methylpyrazinyl) —CH₃ —CH₃ FPD (a, b, and c)-2-(3-methylpyrazinyl) —H —H FPE (a, b, and c) -2-(3-methylpyrazinyl) —H—Cl FPF (a, b, and c) -2-(3-methylpyrazinyl) —H —Br FPG (a, b, and c)-2-(3-methylpyrazinyl) —H —F FPH (a, b, and c) -2-(3-methylpyrazinyl) —H—CH₃ FPI (a, b, and c) -2-(3-methylpyrazinyl) —H —CF₃ FPJ (a, b, and c)-2-(3-methylpyrazinyl) —H —OCH₃ FPK (a, b, and c) -2-(3-methylpyrazinyl)—H —OCH₂CH₃ FPL (a, b, and c) -2-(3-methylpyrazinyl) —H —OCF₃ FPM (a, b,and c) -2-(3-methylpyrazinyl) —H -tert-butyl FPN (a, b, and c)-2-(3-methylpyrazinyl) —H -iso-propyl FPO (a, b, and c) -2-pyridazinyl—Cl —H FPP (a, b, and c) -2-pyridazinyl —Br —H FPQ (a, b, and c)-2-pyridazinyl —F —H FPR (a, b, and c) -2-pyridazinyl —CH₃ —H FPS (a, b,and c) -2-pyridazinyl —CF₃ —H FPT (a, b, and c) -2-pyridazinyl —OCH₃ —HFPU (a, b, and c) -2-pyridazinyl —OCH₂CH₃ —H FPV (a, b, and c)-2-pyridazinyl —OCF₃ —H FPW (a, b, and c) -2-pyridazinyl -tert-butyl —HFPX (a, b, and c) -2-pyridazinyl -iso-propyl —H FPY (a, b, and c)-2-pyridazinyl —CH₃ —CH₃ FPZ (a, b, and c) -2-pyridazinyl —H —H FQA (a,b, and c) -2-pyridazinyl —H —Cl FQB (a, b, and c) -2-pyridazinyl —H —BrFQC (a, b, and c) -2-pyridazinyl —H —F FQD (a, b, and c) -2-pyridazinyl—H —CH₃ FQE (a, b, and c) -2-pyridazinyl —H —CF₃ FQF (a, b, and c)-2-pyridazinyl —H —OCH₃ FQG (a, b, and c) -2-pyridazinyl —H —OCH₂CH₃ FQH(a, b, and c) -2-pyridazinyl —H —OCF₃ FQI (a, b, and c) -2-pyridazinyl—H -tert-butyl FQJ (a, b, and c) -2-pyridazinyl —H -iso-propyl FQK (a,b, and c) -3-(4-chloropyridazinyl) —Cl —H FQL (a, b, and c)-3-(4-chloropyridazinyl) —Br —H FQM (a, b, and c)-3-(4-chloropyridazinyl) —F —H FQN (a, b, and c)-3-(4-chloropyridazinyl) —CH₃ —H FQO (a, b, and c)-3-(4-chloropyridazinyl) —CF₃ —H FQP (a, b, and c)-3-(4-chloropyridazinyl) —OCH₃ —H FQQ (a, b, and c)-3-(4-chloropyridazinyl) —OCH₂CH₃ —H FQR (a, b, and c)-3-(4-chloropyridazinyl) —OCF₃ —H FQS (a, b, and c)-3-(4-chloropyridazinyl) -tert-butyl —H FQT (a, b, and c)-3-(4-chloropyridazinyl) -iso-propyl —H FQU (a, b, and c)-3-(4-chloropyridazinyl) —CH₃ —CH₃ FQV (a, b, and c)-3-(4-chloropyridazinyl) —H —H FQW (a, b, and c)-3-(4-chloropyridazinyl) —H —Cl FQX (a, b, and c)-3-(4-chloropyridazinyl) —H —Br FQY (a, b, and c)-3-(4-chloropyridazinyl) —H —F FQZ (a, b, and c)-3-(4-chloropyridazinyl) —H —CH₃ FRA (a, b, and c)-3-(4-chloropyridazinyl) —H —CF₃ FRB (a, b, and c)-3-(4-chloropyridazinyl) —H —OCH₃ FRC (a, b, and c)-3-(4-chloropyridazinyl) —H —OCH₂CH₃ FRD (a, b, and c)-3-(4-chloropyridazinyl) —H —OCF₃ FRE (a, b, and c)-3-(4-chloropyridazinyl) —H -tert-butyl FRF (a, b, and c)-3-(4-chloropyridazinyl) —H -iso-propyl FRG (a, b, and c)-3-(4-methylpyridazinyl) —Cl —H FRH (a, b, and c)-3-(4-methylpyridazinyl) —Br —H FRI (a, b, and c)-3-(4-methylpyridazinyl) —F —H FRJ (a, b, and c)-3-(4-methylpyridazinyl) —CH₃ —H FRK (a, b, and c)-3-(4-methylpyridazinyl) —CF₃ —H FRL (a, b, and c)-3-(4-methylpyridazinyl) —OCH₃ —H FRM (a, b, and c)-3-(4-methylpyridazinyl) —OCH₂CH₃ —H FRN (a, b, and c)-3-(4-methylpyridazinyl) —OCF₃ —H FRO (a, b, and c)-3-(4-methylpyridazinyl) -tert-butyl —H FRP (a, b, and c)-3-(4-methylpyridazinyl) -iso-propyl —H FRQ (a, b, and c)-3-(4-methylpyridazinyl) —CH₃ —CH₃ FRR (a, b, and c)-3-(4-methylpyridazinyl) —H —H FRS (a, b, and c)-3-(4-methylpyridazinyl) —H —Cl FRT (a, b, and c)-3-(4-methylpyridazinyl) —H —Br FRU (a, b, and c)-3-(4-methylpyridazinyl) —H —F FRV (a, b, and c)-3-(4-methylpyridazinyl) —H —CH₃ FRW (a, b, and c)-3-(4-methylpyridazinyl) —H —CF₃ FRX (a, b, and c)-3-(4-methylpyridazinyl) —H —OCH₃ FRY (a, b, and c)-3-(4-methylpyridazinyl) —H —OCH₂CH₃ FRZ (a, b, and c)-3-(4-methylpyridazinyl) —H —OCF₃ FSA (a, b, and c)-3-(4-methylpyridazinyl) —H -tert-butyl FSB (a, b, and c)-3-(4-methylpyridazinyl) —H -iso-propyl FSC (a, b, and c) -4-thiazanyl—Cl —H FSD (a, b, and c) -4-thiazanyl —Br —H FSE (a, b, and c)-4-thiazanyl —F —H FSF (a, b, and c) -4-thiazanyl —CH₃ —H FSG (a, b, andc) -4-thiazanyl —CF₃ —H FSH (a, b, and c) -4-thiazanyl —OCH₃ —H FSI (a,b, and c) -4-thiazanyl —OCH₂CH₃ —H FSJ (a, b, and c) -4-thiazanyl —OCF₃—H FSK (a, b, and c) -4-thiazanyl -tert-butyl —H FSL (a, b, and c)-4-thiazanyl -iso-propyl —H FSM (a, b, and c) -4-thiazanyl —CH₃ —CH₃ FSN(a, b, and c) -4-thiazanyl —H —H FSO (a, b, and c) -4-thiazanyl —H —ClFSP (a, b, and c) -4-thiazanyl —H —Br FSQ (a, b, and c) -4-thiazanyl —H—F FSR (a, b, and c) -4-thiazanyl —H —CH₃ FSS (a, b, and c) -4-thiazanyl—H —CF₃ FST (a, b, and c) -4-thiazanyl —H —OCH₃ FSU (a, b, and c)-4-thiazanyl —H —OCH₂CH₃ FSV (a, b, and c) -4-thiazanyl —H —OCF₃ FSW (a,b, and c) -4-thiazanyl —H -tert-butyl FSX (a, b, and c) -4-thiazanyl —H-iso-propyl FSY (a, b, and c) -5-(4-chlorothiazanyl) —Cl —H FSZ (a, b,and c) -5-(4-chlorothiazanyl) —Br —H FTA (a, b, and c)-5-(4-chlorothiazanyl) —F —H FTB (a, b, and c) -5-(4-chlorothiazanyl)—CH₃ —H FTC (a, b, and c) -5-(4-chlorothiazanyl) —CF₃ —H FTD (a, b, andc) -5-(4-chlorothiazanyl) —OCH₃ —H FTE (a, b, and c)-5-(4-chlorothiazanyl) —OCH₂CH₃ —H FTF (a, b, and c)-5-(4-chlorothiazanyl) —OCF₃ —H FTG (a, b, and c) -5-(4-chlorothiazanyl)-tert-butyl —H FTH (a, b, and c) -5-(4-chlorothiazanyl) -iso-propyl —HFTI (a, b, and c) -5-(4-chlorothiazanyl) —CH₃ —CH₃ FTJ (a, b, and c)-5-(4-chlorothiazanyl) —H —H FTK (a, b, and c) -5-(4-chlorothiazanyl) —H—Cl FTL (a, b, and c) -5-(4-chlorothiazanyl) —H —Br FTM (a, b, and c)-5-(4-chlorothiazanyl) —H —F FTN (a, b, and c) -5-(4-chlorothiazanyl) —H—CH₃ FTO (a, b, and c) -5-(4-chlorothiazanyl) —H —CF₃ FTP (a, b, and c)-5-(4-chlorothiazanyl) —H —OCH₃ FTQ (a, b, and c) -5-(4-chlorothiazanyl)—H —OCH₂CH₃ FTR (a, b, and c) -5-(4-chlorothiazanyl) —H —OCF₃ FTS (a, b,and c) -5-(4-chlorothiazanyl) —H -tert-butyl FTT (a, b, and c)-5-(4-chlorothiazanyl) —H -iso-propyl FTU (a, b, and c)-5-(4-methylthiazanyl) —Cl —H FTV (a, b, and c) -5-(4-methylthiazanyl)—Br —H FTW (a, b, and c) -5-(4-methylthiazanyl) —F —H FTX (a, b, and c)-5-(4-methylthiazanyl) —CH₃ —H FTY (a, b, and c) -5-(4-methylthiazanyl)—CF₃ —H FTZ (a, b, and c) -5-(4-methylthiazanyl) —OCH₃ —H FUA (a, b, andc) -5-(4-methylthiazanyl) —OCH₂CH₃ —H FUB (a, b, and c)-5-(4-methylthiazanyl) —OCF₃ —H FUC (a, b, and c) -5-(4-methylthiazanyl)-tert-butyl —H FUD (a, b, and c) -5-(4-methylthiazanyl) -iso-propyl —HFUE (a, b, and c) -5-(4-methylthiazanyl) —CH₃ —CH₃ FUF (a, b, and c)-5-(4-methylthiazanyl) —H —H FUG (a, b, and c) -5-(4-methylthiazanyl) —H—Cl FUH (a, b, and c) -5-(4-methylthiazanyl) —H —Br FUI (a, b, and c)-5-(4-methylthiazanyl) —H —F FUJ (a, b, and c) -5-(4-methylthiazanyl) —H—CH₃ FUK (a, b, and c) -5-(4-methylthiazanyl) —H —CF₃ FUL (a, b, and c)-5-(4-methylthiazanyl) —H —OCH₃ FUM (a, b, and c) -5-(4-methylthiazanyl)—H —OCH₂CH₃ FUN (a, b, and c) -5-(4-methylthiazanyl) —H —OCF₃ FUO (a, b,and c) -5-(4-methylthiazanyl) —H -tert-butyl FUP (a, b, and c)-5-(4-methylthiazanyl) —H -iso-propyl “a” means theBenzoazolylpiperazine Compound is racemic. “b” means the carbon atom ofthe piperazine ring attached to the methyl group is in the Rconfiguration. “c” means the carbon atom of the piperazine ring attachedto the methyl group is in the S configuration.

TABLE XVI

and pharmaceutically acceptable salts thereof, wherein: Compound Ar₁ R₈R₉ FUQ (a, b, and c) -2-(3-chloropyridyl) —Cl —H FUR (a, b, and c)-2-(3-chloropyridyl) —Br —H FUS (a, b, and c) -2-(3-chloropyridyl) —F —HFUT (a, b, and c) -2-(3-chloropyridyl) —CH₃ —H FUU (a, b, and c)-2-(3-chloropyridyl) —CF₃ —H FUV (a, b, and c) -2-(3-chloropyridyl)—OCH₃ —H FUW (a, b, and c) -2-(3-chloropyridyl) —OCH₂CH₃ —H FUX (a, b,and c) -2-(3-chloropyridyl) —OCF₃ —H FUY (a, b, and c)-2-(3-chloropyridyl) -tert-butyl —H FUZ (a, b, and c)-2-(3-chloropyridyl) -iso-propyl —H FVA (a, b, and c)-2-(3-chloropyridyl) —CH₃ —CH₃ FVB (a, b, and c) -2-(3-chloropyridyl) —H—H FVC (a, b, and c) -2-(3-chloropyridyl) —H —Cl FVD (a, b, and c)-2-(3-chloropyridyl) —H —Br FVE (a, b, and c) -2-(3-chloropyridyl) —H —FFVF (a, b, and c) -2-(3-chloropyridyl) —H —CH₃ FVG (a, b, and c)-2-(3-chloropyridyl) —H —CF₃ FVH (a, b, and c) -2-(3-chloropyridyl) —H—OCH₃ FVI (a, b, and c) -2-(3-chloropyridyl) —H —OCH₂CH₃ FVJ (a, b, andc) -2-(3-chloropyridyl) —H —OCF₃ FVK (a, b, and c) -2-(3-chloropyridyl)—H -tert-butyl FVL (a, b, and c) -2-(3-chloropyridyl) —H -iso-propyl FVM(a, b, and c) -2-(3-methylpyridyl) —Cl —H FVN (a, b, and c)-2-(3-methylpyridyl) —Br —H FVO (a, b, and c) -2-(3-methylpyridyl) —F —HFVP (a, b, and c) -2-(3-methylpyridyl) —CH₃ —H FVQ (a, b, and c)-2-(3-methylpyridyl) —CF₃ —H FVR (a, b, and c) -2-(3-methylpyridyl)—OCH₃ —H FVS (a, b, and c) -2-(3-methylpyridyl) —OCH₂CH₃ —H FVT (a, b,and c) -2-(3-methylpyridyl) —OCF₃ —H FVU (a, b, and c)-2-(3-methylpyridyl) -tert-butyl —H FVV (a, b, and c)-2-(3-methylpyridyl) -iso-propyl —H FVW (a, b, and c)-2-(3-methylpyridyl) —CH₃ —CH₃ FVX (a, b, and c) -2-(3-methylpyridyl) —H—H FVY (a, b, and c) -2-(3-methylpyridyl) —H —Cl FVZ (a, b, and c)-2-(3-methylpyridyl) —H —Br FWA (a, b, and c) -2-(3-methylpyridyl) —H —FFWB (a, b, and c) -2-(3-methylpyridyl) —H —CH₃ FWC (a, b, and c)-2-(3-methylpyridyl) —H —CF₃ FWD (a, b, and c) -2-(3-methylpyridyl) —H—OCH₃ FWE (a, b, and c) -2-(3-methylpyridyl) —H —OCH₂CH₃ FWF (a, b, andc) -2-(3-methylpyridyl) —H —OCF₃ FWG (a, b, and c) -2-(3-methylpyridyl)—H -tert-butyl FWH (a, b, and c) -2-(3-methylpyridyl) —H -iso-propyl FWI(a, b, and c) -2-(3-CF₃-pyridyl) —Cl —H FWJ (a, b, and c)-2-(3-CF₃-pyridyl) —Br —H FWK (a, b, and c) -2-(3-CF₃-pyridyl) —F —H FWL(a, b, and c) -2-(3-CF₃-pyridyl) —CH₃ —H FWM -2-(3-CF₃-pyridyl) —CF₃ —H(a, b, and c) FWN (a, b, and c) -2-(3-CF₃-pyridyl) —OCH₃ —H FWO (a, b,and c) -2-(3-CF₃-pyridyl) —OCH₂CH₃ —H FWP (a, b, and c)-2-(3-CF₃-pyridyl) —OCF₃ —H FWQ (a, b, and c) -2-(3-CF₃-pyridyl)-tert-butyl —H FWR (a, b, and c) -2-(3-CF₃-pyridyl) -iso-propyl —H FWS(a, b, and c) -2-(3-CF₃-pyridyl) —CH₃ —CH₃ FWT (a, b, and c)-2-(3-CF₃-pyridyl) —H —H FWU (a, b, and c) -2-(3-CF₃-pyridyl) —H —Cl FWV(a, b, and c) -2-(3-CF₃-pyridyl) —H —Br FWW -2-(3-CF₃-pyridyl) —H —F (a,b, and c) FWX (a, b, and c) -2-(3-CF₃-pyridyl) —H —CH₃ FWY (a, b, and c)-2-(3-CF₃-pyridyl) —H —CF₃ FWZ (a, b, and c) -2-(3-CF₃-pyridyl) —H —OCH₃FXA (a, b, and c) -2-(3-CF₃-pyridyl) —H —OCH₂CH₃ FXB (a, b, and c)-2-(3-CF₃-pyridyl) —H —OCF₃ FXC (a, b, and c) -2-(3-CF₃-pyridyl) —H-tert-butyl FXD (a, b, and c) -2-(3-CF₃-pyridyl) —H -iso-propyl FXE (a,b, and c) -4-(5-chloropyrimidinyl) —Cl —H FXF (a, b, and c)-4-(5-chloropyrimidinyl) —Br —H FXG (a, b, and c)-4-(5-chloropyrimidinyl) —F —H FXH (a, b, and c)-4-(5-chloropyrimidinyl) —CH₃ —H FXI (a, b, and c)-4-(5-chloropyrimidinyl) —CF₃ —H FXJ (a, b, and c)-4-(5-chloropyrimidinyl) —OCH₃ —H FXK (a, b, and c)-4-(5-chloropyrimidinyl) —OCH₂CH₃ —H FXL (a, b, and c)-4-(5-chloropyrimidinyl) —OCF₃ —H FXM (a, b, and c)-4-(5-chloropyrimidinyl) -tert-butyl —H FXN (a, b, and c)-4-(5-chloropyrimidinyl) -iso-propyl —H FXO (a, b, and c)-4-(5-chloropyrimidinyl) —CH₃ —CH₃ FXP (a, b, and c)-4-(5-chloropyrimidinyl) —H —H FXQ (a, b, and c)-4-(5-chloropyrimidinyl) —H —Cl FXR (a, b, and c)-4-(5-chloropyrimidinyl) —H —Br FXS (a, b, and c)-4-(5-chloropyrimidinyl) —H —F FXT (a, b, and c)-4-(5-chloropyrimidinyl) —H —CH₃ FXU (a, b, and c)-4-(5-chloropyrimidinyl) —H —CF₃ FXV (a, b, and c)-4-(5-chloropyrimidinyl) —H —OCH₃ FXW (a, b, and c)-4-(5-chloropyrimidinyl) —H —OCH₂CH₃ FXX (a, b, and c)-4-(5-chloropyrimidinyl) —H —OCF₃ FXY (a, b, and c)-4-(5-chloropyrimidinyl) —H -tert-butyl FXZ (a, b, and c)-4-(5-chloropyrimidinyl) —H -iso-propyl FYA (a, b, and c)-4-(5-methylpyrimidinyl) —Cl —H FYB (a, b, and c)-4-(5-methylpyrimidinyl) —Br —H FYC (a, b, and c)-4-(5-methylpyrimidinyl) —F —H FYD (a, b, and c)-4-(5-methylpyrimidinyl) —CH₃ —H FYE (a, b, and c)-4-(5-methylpyrimidinyl) —CF₃ —H FYF (a, b, and c)-4-(5-methylpyrimidinyl) —OCH₃ —H FYG (a, b, and c)-4-(5-methylpyrimidinyl) —OCH₂CH₃ —H FYH (a, b, and c)-4-(5-methylpyrimidinyl) —OCF₃ —H FYI (a, b, and c)-4-(5-methylpyrimidinyl) -tert-butyl —H FYJ (a, b, and c)-4-(5-methylpyrimidinyl) -iso-propyl —H FYK (a, b, and c)-4-(5-methylpyrimidinyl) —CH₃ —CH₃ FYL (a, b, and c)-4-(5-methylpyrimidinyl) —H —H FYM (a, b, and c)-4-(5-methylpyrimidinyl) —H —Cl FYN (a, b, and c)-4-(5-methylpyrimidinyl) —H —Br FYO (a, b, and c)-4-(5-methylpyrimidinyl) —H —F FYP (a, b, and c)-4-(5-methylpyrimidinyl) —H —CH₃ FYQ (a, b, and c)-4-(5-methylpyrimidinyl) —H —CF₃ FYR (a, b, and c)-4-(5-methylpyrimidinyl) —H —OCH₃ FYS (a, b, and c)-4-(5-methylpyrimidinyl) —H —OCH₂CH₃ FYT (a, b, and c)-4-(5-methylpyrimidinyl) —H —OCF₃ FYU (a, b, and c)-4-(5-methylpyrimidinyl) —H -tert-butyl FYV (a, b, and c)-4-(5-methylpyrimidinyl) —H -iso-propyl FYW (a, b, and c) -2-pyrazinyl—Cl —H FYX (a, b, and c) -2-pyrazinyl —Br —H FYY (a, b, and c)-2-pyrazinyl —F —H FYZ (a, b, and c) -2-pyrazinyl —CH₃ —H FZA (a, b, andc) -2-pyrazinyl —CF₃ —H FZB (a, b, and c) -2-pyrazinyl —OCH₃ —H FZC (a,b, and c) -2-pyrazinyl —OCH₂CH₃ —H FZD (a, b, and c) -2-pyrazinyl —OCF₃—H FZE (a, b, and c) -2-pyrazinyl -tert-butyl —H FZF (a, b, and c)-2-pyrazinyl -iso-propyl —H FZG (a, b, and c) -2-pyrazinyl —CH₃ —CH₃ FZH(a, b, and c) -2-pyrazinyl —H —H FZI (a, b, and c) -2-pyrazinyl —H —ClFZJ (a, b, and c) -2-pyrazinyl —H —Br FZK (a, b, and c) -2-pyrazinyl —H—F FZL (a, b, and c) -2-pyrazinyl —H —CH₃ FZM (a, b, and c) -2-pyrazinyl—H —CF₃ FZN (a, b, and c) -2-pyrazinyl —H —OCH₃ FZO (a, b, and c)-2-pyrazinyl —H —OCH₂CH₃ FZP (a, b, and c) -2-pyrazinyl —H —OCF₃ FZQ (a,b, and c) -2-pyrazinyl —H -tert-butyl FZR (a, b, and c) -2-pyrazinyl —H-iso-propyl FZS (a, b, and c) -2-(3-chloropyrazinyl) —Cl —H FZT (a, b,and c) -2-(3-chloropyrazinyl) —Br —H FZU (a, b, and c)-2-(3-chloropyrazinyl) —F —H FZV (a, b, and c) -2-(3-chloropyrazinyl)—CH₃ —H FZW (a, b, and c) -2-(3-chloropyrazinyl) —CF₃ —H FZX (a, b, andc) -2-(3-chloropyrazinyl) —OCH₃ —H FZY (a, b, and c)-2-(3-chloropyrazinyl) —OCH₂CH₃ —H FZZ (a, b, and c)-2-(3-chloropyrazinyl) —OCF₃ —H GAA (a, b, and c) -2-(3-chloropyrazinyl)-tert-butyl —H GAB (a, b, and c) -2-(3-chloropyrazinyl) -iso-propyl —HGAC (a, b, and c) -2-(3-chloropyrazinyl) —CH₃ —CH₃ GAD (a, b, and c)-2-(3-chloropyrazinyl) —H —H GAE (a, b, and c) -2-(3-chloropyrazinyl) —H—Cl GAF (a, b, and c) -2-(3-chloropyrazinyl) —H —Br GAG (a, b, and c)-2-(3-chloropyrazinyl) —H —F GAH (a, b, and c) -2-(3-chloropyrazinyl) —H—CH₃ GAI (a, b, and c) -2-(3-chloropyrazinyl) —H —CF₃ GAJ (a, b, and c)-2-(3-chloropyrazinyl) —H —OCH₃ GAK (a, b, and c) -2-(3-chloropyrazinyl)—H —OCH₂CH₃ GAL (a, b, and c) -2-(3-chloropyrazinyl) —H —OCF₃ GAM-2-(3-chloropyrazinyl) —H -tert-butyl (a, b, and c) GAN (a, b, and c)-2-(3-chloropyrazinyl) —H -iso-propyl GAO (a, b, and c)-2-(3-methylpyrazinyl) —Cl —H GAP (a, b, and c) -2-(3-methylpyrazinyl)—Br —H GAQ (a, b, and c) -2-(3-methylpyrazinyl) —F —H GAR (a, b, and c)-2-(3-methylpyrazinyl) —CH₃ —H GAS (a, b, and c) -2-(3-methylpyrazinyl)—CF₃ —H GAT (a, b, and c) -2-(3-methylpyrazinyl) —OCH₃ —H GAU (a, b, andc) -2-(3-methylpyrazinyl) —OCH₂CH₃ —H GAV (a, b, and c)-2-(3-methylpyrazinyl) —OCF₃ —H GAW -2-(3-methylpyrazinyl) -tert-butyl—H (a, b, and c) GAX (a, b, and c) -2-(3-methylpyrazinyl) -iso-propyl —HGAY (a, b, and c) -2-(3-methylpyrazinyl) —CH₃ —CH₃ GAZ (a, b, and c)-2-(3-methylpyrazinyl) —H —H GBA (a, b, and c) -2-(3-methylpyrazinyl) —H—Cl GBB (a, b, and c) -2-(3-methylpyrazinyl) —H —Br GBC (a, b, and c)-2-(3-methylpyrazinyl) —H —F GBD (a, b, and c) -2-(3-methylpyrazinyl) —H—CH₃ GBE (a, b, and c) -2-(3-methylpyrazinyl) —H —CF₃ GBF (a, b, and c)-2-(3-methylpyrazinyl) —H —OCH₃ GBG (a, b, and c) -2-(3-methylpyrazinyl)—H —OCH₂CH₃ GBH (a, b, and c) -2-(3-methylpyrazinyl) —H —OCF₃ GBI (a, b,and c) -2-(3-methylpyrazinyl) —H -tert-butyl GBJ (a, b, and c)-2-(3-methylpyrazinyl) —H -iso-propyl GBK (a, b, and c) -2-pyridazinyl—Cl —H GBL (a, b, and c) -2-pyridazinyl —Br —H GBM -2-pyridazinyl —F —H(a, b, and c) GBN (a, b, and c) -2-pyridazinyl —CH₃ —H GBO (a, b, and c)-2-pyridazinyl —CF₃ —H GBP (a, b, and c) -2-pyridazinyl —OCH₃ —H GBQ (a,b, and c) -2-pyridazinyl —OCH₂CH₃ —H GBR (a, b, and c) -2-pyridazinyl—OCF₃ —H GBS (a, b, and c) -2-pyridazinyl -tert-butyl —H GBT (a, b, andc) -2-pyridazinyl -iso-propyl —H GBU (a, b, and c) -2-pyridazinyl —CH₃—CH₃ GBV (a, b, and c) -2-pyridazinyl —H —H GBW -2-pyridazinyl —H —Cl(a, b, and c) GBX (a, b, and c) -2-pyridazinyl —H —Br GBY (a, b, and c)-2-pyridazinyl —H —F GBZ (a, b, and c) -2-pyridazinyl —H —CH₃ GCA (a, b,and c) -2-pyridazinyl —H —CF₃ GCB (a, b, and c) -2-pyridazinyl —H —OCH₃GCC (a, b, and c) -2-pyridazinyl —H —OCH₂CH₃ GCD (a, b, and c)-2-pyridazinyl —H —OCF₃ GCE (a, b, and c) -2-pyridazinyl —H -tert-butylGCF (a, b, and c) -2-pyridazinyl —H -iso-propyl GCG (a, b, and c)-3-(4-chloropyridazinyl) —Cl —H GCH (a, b, and c)-3-(4-chloropyridazinyl) —Br —H GCI (a, b, and c)-3-(4-chloropyridazinyl) —F —H GCJ (a, b, and c)-3-(4-chloropyridazinyl) —CH₃ —H GCK (a, b, and c)-3-(4-chloropyridazinyl) —CF₃ —H GCL (a, b, and c)-3-(4-chloropyridazinyl) —OCH₃ —H GCM -3-(4-chloropyridazinyl) —OCH₂CH₃—H (a, b, and c) GCN (a, b, and c) -3-(4-chloropyridazinyl) —OCF₃ —H GCO(a, b, and c) -3-(4-chloropyridazinyl) -tert-butyl —H GCP (a, b, and c)-3-(4-chloropyridazinyl) -iso-propyl —H GCQ (a, b, and c)-3-(4-chloropyridazinyl) —CH₃ —CH₃ GCR (a, b, and c)-3-(4-chloropyridazinyl) —H —H GCS (a, b, and c)-3-(4-chloropyridazinyl) —H —Cl GCT (a, b, and c)-3-(4-chloropyridazinyl) —H —Br GCU (a, b, and c)-3-(4-chloropyridazinyl) —H —F GCV (a, b, and c)-3-(4-chloropyridazinyl) —H —CH₃ GCW -3-(4-chloropyridazinyl) —H —CF₃(a, b, and c) GCX (a, b, and c) -3-(4-chloropyridazinyl) —H —OCH₃ GCY(a, b, and c) -3-(4-chloropyridazinyl) —H —OCH₂CH₃ GCZ (a, b, and c)-3-(4-chloropyridazinyl) —H —OCF₃ GDA (a, b, and c)-3-(4-chloropyridazinyl) —H -tert-butyl GDB (a, b, and c)-3-(4-chloropyridazinyl) —H -iso-propyl GDC (a, b, and c)-3-(4-methylpyridazinyl) —Cl —H GDD (a, b, and c)-3-(4-methylpyridazinyl) —Br —H GDE (a, b, and c)-3-(4-methylpyridazinyl) —F —H GDF (a, b, and c)-3-(4-methylpyridazinyl) —CH₃ —H GDG (a, b, and c)-3-(4-methylpyridazinyl) —CF₃ —H GDH (a, b, and c)-3-(4-methylpyridazinyl) —OCH₃ —H GDI (a, b, and c)-3-(4-methylpyridazinyl) —OCH₂CH₃ —H GDJ (a, b, and c)-3-(4-methylpyridazinyl) —OCF₃ —H GDK (a, b, and c)-3-(4-methylpyridazinyl) -tert-butyl —H GDL (a, b, and c)-3-(4-methylpyridazinyl) -iso-propyl —H GDM -3-(4-methylpyridazinyl)—CH₃ —CH₃ (a, b, and c) GDN (a, b, and c) -3-(4-methylpyridazinyl) —H —HGDO (a, b, and c) -3-(4-methylpyridazinyl) —H —Cl GDP (a, b, and c)-3-(4-methylpyridazinyl) —H —Br GDQ (a, b, and c)-3-(4-methylpyridazinyl) —H —F GDR (a, b, and c)-3-(4-methylpyridazinyl) —H —CH₃ GDS (a, b, and c)-3-(4-methylpyridazinyl) —H —CF₃ GDT (a, b, and c)-3-(4-methylpyridazinyl) —H —OCH₃ GDU (a, b, and c)-3-(4-methylpyridazinyl) —H —OCH₂CH₃ GDV (a, b, and c)-3-(4-methylpyridazinyl) —H —OCF₃ GDW -3-(4-methylpyridazinyl) —H-tert-butyl (a, b, and c) GDX (a, b, and c) -3-(4-methylpyridazinyl) —H-iso-propyl GDY (a, b, and c) -4-thiazanyl —Cl —H GDZ (a, b, and c)-4-thiazanyl —Br —H GEA (a, b, and c) -4-thiazanyl —F —H GEB (a, b, andc) -4-thiazanyl —CH₃ —H GEC (a, b, and c) -4-thiazanyl —CF₃ —H GED (a,b, and c) -4-thiazanyl —OCH₃ —H GEE (a, b, and c) -4-thiazanyl —OCH₂CH₃—H GEF (a, b, and c) -4-thiazanyl —OCF₃ —H GEG (a, b, and c)-4-thiazanyl -tert-butyl —H GEH (a, b, and c) -4-thiazanyl -iso-propyl—H GEI (a, b, and c) -4-thiazanyl —CH₃ —CH₃ GEJ (a, b, and c)-4-thiazanyl —H —H GEK (a, b, and c) -4-thiazanyl —H —Cl GEL (a, b, andc) -4-thiazanyl —H —Br GEM (a, b, and c) -4-thiazanyl —H —F GEN (a, b,and c) -4-thiazanyl —H —CH₃ GEO (a, b, and c) -4-thiazanyl —H —CF₃ GEP(a, b, and c) -4-thiazanyl —H —OCH₃ GEQ (a, b, and c) -4-thiazanyl —H—OCH₂CH₃ GER (a, b, and c) -4-thiazanyl —H —OCF₃ GES (a, b, and c)-4-thiazanyl —H -tert-butyl GET (a, b, and c) -4-thiazanyl —H-iso-propyl GEU (a, b, and c) -5-(4-chlorothiazanyl) —Cl —H GEV (a, b,and c) -5-(4-chlorothiazanyl) —Br —H GEW -5-(4-chlorothiazanyl) —F —H(a, b, and c) GEX (a, b, and c) -5-(4-chlorothiazanyl) —CH₃ —H GEY (a,b, and c) -5-(4-chlorothiazanyl) —CF₃ —H GEZ (a, b, and c)-5-(4-chlorothiazanyl) —OCH₃ —H GFA (a, b, and c) -5-(4-chlorothiazanyl)—OCH₂CH₃ —H GFB (a, b, and c) -5-(4-chlorothiazanyl) —OCF₃ —H GFC (a, b,and c) -5-(4-chlorothiazanyl) -tert-butyl —H GFD (a, b, and c)-5-(4-chlorothiazanyl) -iso-propyl —H GFE (a, b, and c)-5-(4-chlorothiazanyl) —CH₃ —CH₃ GFF (a, b, and c)-5-(4-chlorothiazanyl) —H —H GFG (a, b, and c) -5-(4-chlorothiazanyl) —H—Cl GFH (a, b, and c) -5-(4-chlorothiazanyl) —H —Br GFI (a, b, and c)-5-(4-chlorothiazanyl) —H —F GFJ (a, b, and c) -5-(4-chlorothiazanyl) —H—CH₃ GFK (a, b, and c) -5-(4-chlorothiazanyl) —H —CF₃ GFL (a, b, and c)-5-(4-chlorothiazanyl) —H —OCH₃ GFM (a, b, and c) -5-(4-chlorothiazanyl)—H —OCH₂CH₃ GFN (a, b, and c) -5-(4-chlorothiazanyl) —H —OCF₃ GFO (a, b,and c) -5-(4-chlorothiazanyl) —H -tert-butyl GFP (a, b, and c)-5-(4-chlorothiazanyl) —H -iso-propyl GFQ (a, b, and c)-5-(4-methylthiazanyl) —Cl —H GFR (a, b, and c) -5-(4-methylthiazanyl)—Br —H GFS (a, b, and c) -5-(4-methylthiazanyl) —F —H GFT (a, b, and c)-5-(4-methylthiazanyl) —CH₃ —H GFU (a, b, and c) -5-(4-methylthiazanyl)—CF₃ —H GFV (a, b, and c) -5-(4-methylthiazanyl) —OCH₃ —H GFW (a, b, andc) -5-(4-methylthiazanyl) —OCH₂CH₃ —H GFX (a, b, and c)-5-(4-methylthiazanyl) —OCF₃ —H GFY (a, b, and c) -5-(4-methylthiazanyl)-tert-butyl —H GFZ (a, b, and c) -5-(4-methylthiazanyl) -iso-propyl —HGGA (a, b, and c) -5-(4-methylthiazanyl) —CH₃ —CH₃ GGB (a, b, and c)-5-(4-methylthiazanyl) —H —H GGC (a, b, and c) -5-(4-methylthiazanyl) —H—Cl GGD (a, b, and c) -5-(4-methylthiazanyl) —H —Br GGE (a, b, and c)-5-(4-methylthiazanyl) —H —F GGF (a, b, and c) -5-(4-methylthiazanyl) —H—CH₃ GGG (a, b, and c) -5-(4-methylthiazanyl) —H —CF₃ GGH (a, b, and c)-5-(4-methylthiazanyl) —H —OCH₃ GGI (a, b, and c) -5-(4-methylthiazanyl)—H —OCH₂CH₃ GGJ (a, b, and c) -5-(4-methylthiazanyl) —H —OCF₃ GGK (a, b,and c) -5-(4-methylthiazanyl) —H -tert-butyl GGL (a, b, and c)-5-(4-methylthiazanyl) —H -iso-propyl “a” means theBenzoazolylpiperazine Compound is racemic. “b” means the carbon atom ofthe piperazine ring attached to the methyl group is in the Rconfiguration. “c” means the carbon atom of the piperazine ring attachedto the methyl group is in the S configuration.

TABLE XIX

and pharmaceutically acceptable salts thereof, wherein: Compound X R₈ R₉GGM S —Cl —H GGN S —Br —H GGO S —F —H GGP S —CH₃ —H GGQ S —CF₃ —H GGR S—OCH₃ —H GGS S —OCH₂CH₃ —H GGT S —OCF₃ —H GGU S -tert-butyl —H GGV S-iso-propyl —H GGW S —CH₃ —CH₃ GGX S —H —H GGY S —H —Cl GGZ S —H —Br GHAS —H —F GHB S —H —CH₃ GHC S —H —CF₃ GHD S —H —OCH₃ GHE S —H —OCH₂CH₃ GHFS —H —OCF₃ GHG S —H -tert-butyl GHH S —H -iso-propyl GHI O —Cl —H GHJ O—Br —H GHK O —F —H GHL O —CH₃ —H GHM O —CF₃ —H GHN O —OCH₃ —H GHO O—OCH₂CH₃ —H GHP O —OCF₃ —H GHQ O -tert-butyl —H GHR O -iso-propyl —H GHSO —CH₃ —CH₃ GHT O —H —H GHU O —H —Cl GHV O —H —Br GHW O —H —F GHX O —H—CH₃ GHY O —H —CF₃ GHZ O —H —OCH₃ GIA O —H —OCH₂CH₃ GIB O —H —OCF₃ GIC O—H -tert-butyl GID O —H -iso-propyl GIE NH —Cl —H GIF NH —Br —H GIG NH—F —H GIH NH —CH₃ —H GII NH —CF₃ —H GIJ NH —OCH₃ —H GIK NH —OCH₂CH₃ —HGIL NH —OCF₃ —H GIM NH -tert-butyl —H GIN NH -iso-propyl —H GIO NH —CH₃—CH₃ GIP NH —H —H GIQ NH —H —Cl GIR NH —H —Br GIS NH —H —F GIT NH —H—CH₃ GIU NH —H —CF₃ GIV NH —H —OCH₃ GIW NH —H —OCH₂CH₃ GIX NH —H —OCF₃GIY NH —H -tert-butyl GIZ NH —H -iso-propyl

TABLE XX

and pharmaceutically acceptable salts thereof, wherein: Compound X R₈ R₉GJA S —Cl —H GJB S —Br —H GJC S —F —H GJD S —CH₃ —H GJE S —CF₃ —H GJF S—OCH₃ —H GJG S —OCH₂CH₃ —H GJH S —OCF₃ —H GJI S -tert-butyl —H GJJ S-iso-propyl —H GJK S —CH₃ —CH₃ GJL S —H —H GJM S —H —Cl GJN S —H —Br GJOS —H —F GJP S —H —CH₃ GJQ S —H —CF₃ GJR S —H —OCH₃ GJS S —H —OCH₂CH₃ GJTS —H —OCF₃ GJU S —H -tert-butyl GJV S —H -iso-propyl GJW O —Cl —H GJX O—Br —H GJY O —F —H GJZ O —CH₃ —H GKA O —CF₃ —H GKB O —OCH₃ —H GKC O—OCH₂CH₃ —H GKD O —OCF₃ —H GKE O -tert-butyl —H GKF O -iso-propyl —H GKGO —CH₃ —CH₃ GKH O —H —H GKJ O —H —Cl GKJ O —H —Br GKK O —H —F GKL O —H—CH₃ GKM O —H —CF₃ GKN O —H —OCH₃ GKO O —H —OCH₂CH₃ GKP O —H —OCF₃ GKQ O—H -tert-butyl GKR O —H -iso-propyl GKS N —Cl —H GKT N —Br —H GKU N —F—H GKV N —CH₃ —H GKW N —CF₃ —H GKX N —OCH₃ —H GKY N —OCH₂CH₃ —H GKZ N—OCF₃ —H GLA N -tert-butyl —H GLB N -iso-propyl —H GLC N —CH₃ —CH₃ GLD N—H —H GLE N —H —Cl GLF N —H —Br GLG N —H —F GLH N —H —CH₃ GLI N —H —CF₃GLJ N —H —OCH₃ GLK N —H —OCH₂CH₃ GLL N —H —OCF₃ GLM N —H -tert-butyl GLNN —H -iso-propyl

TABLE XXI

and pharmaceutically acceptable salts thereof, wherein: Compound X R₁ R₂R₉ GLO S —CH₃ —Cl —F GLP S —CH₃ —Cl —Cl GLQ S —CH₃ —Cl —CH₃ GLR S —CH₃—F —F GLS S —CH₃ —F —Cl GLT S —CH₃ —F —CH₃ GLU S —CF₃ —Cl —F GLV S —CF₃—Cl —Cl GLW S —CF₃ —Cl —CH₃ GLX S —CF₃ —F —F GLY S —CF₃ —F —Cl GLZ S—CF₃ —F —CH₃ GMA S —Cl —Cl —F GMB S —Cl —Cl —Cl GMC S —Cl —Cl —CH₃ GMD S—Cl —F —F GME S —Cl —F —Cl GMF S —Cl —F —CH₃ GMG NH —CH₃ —Cl —F GMH NH—CH₃ —Cl —Cl GMI NH —CH₃ —Cl —CH₃ GMJ NH —CH₃ —F —F GMK NH —CH₃ —F —ClGML NH —CH₃ —F —CH₃ GMM NH —CF₃ —Cl —F GMN NH —CF₃ —Cl —Cl GMO NH —CF₃—Cl —CH₃ GMP NH —CF₃ —F —F GMQ NH —CF₃ —F —Cl GMR NH —CF₃ —F —CH₃ GMS NH—Cl —Cl —F GMT NH —Cl —Cl —Cl GMU NH —Cl —Cl —CH₃ GMV NH —Cl —F —F GMWNH —Cl —F —Cl GMX NH —Cl —F —CH₃ GMY O —CH₃ —Cl —F GMZ O —CH₃ —Cl —ClGNA O —CH₃ —Cl —CH₃ GNB O —CH₃ —F —F GNC O —CH₃ —F —Cl GND O —CH₃ —F—CH₃ GNE O —CF₃ —Cl —F GNF O —CF₃ —Cl —Cl GNG O —CF₃ —Cl —CH₃ GNH O —CF₃—F —F GNI O —CF₃ —F —Cl GNJ O —CF₃ —F —CH₃ GNK O —Cl —Cl —F GNL O —Cl—Cl —Cl GNM O —Cl —Cl —CH₃ GNN O —Cl —F —F GNO O —Cl —F —Cl GNP O —Cl —F—CH₃

TABLE XXII

and pharmaceutically acceptable salts thereof, wherein: Compound X R₁ R₂R₉ GNQ S —CH₃ —Cl —F GNR S —CH₃ —Cl —Cl GNS S —CH₃ —Cl —CH₃ GNT S —CH₃—F —F GNU S —CH₃ —F —Cl GNV S —CH₃ —F —CH₃ GNW S —CF₃ —Cl —F GNX S —CF₃—Cl —Cl GNY S —CF₃ —Cl —CH₃ GNZ S —CF₃ —F —F GOA S —CF₃ —F —Cl GOB S—CF₃ —F —CH₃ GOC S —Cl —Cl —F GOD S —Cl —Cl —Cl GOE S —Cl —Cl —CH₃ GOF S—Cl —F —F GOG S —Cl —F —Cl GOH S —Cl —F —CH₃ GOI NH —CH₃ —Cl —F GOJ NH—CH₃ —Cl —Cl GOK NH —CH₃ —Cl —CH₃ GOL NH —CH₃ —F —F GOM NH —CH₃ —F —ClGON NH —CH₃ —F —CH₃ GOO NH —CF₃ —Cl —F GOP NH —CF₃ —Cl —Cl GOQ NH —CF₃—Cl —CH₃ GOR NH —CF₃ —F —F GOS NH —CF₃ —F —Cl GOT NH —CF₃ —F —CH₃ GOU NH—Cl —Cl —F GOV NH —Cl —Cl —Cl GOW NH —Cl —Cl —CH₃ GOX NH —Cl —F —F GOYNH —Cl —F —Cl GOZ NH —Cl —F —CH₃ GPA O —CH₃ —Cl —F GPB O —CH₃ —Cl —ClGPC O —CH₃ —Cl —CH₃ GPD O —CH₃ —F —F GPE O —CH₃ —F —Cl GPF O —CH₃ —F—CH₃ GPG O —CF₃ —Cl —F GPH O —CF₃ —Cl —Cl GPI O —CF₃ —Cl —CH₃ GPJ O —CF₃—F —F GPK O —CF₃ —F —Cl GPL O —CF₃ —F —CH₃ GPM O —Cl —Cl —F GPN O —Cl—Cl —Cl GPO O —Cl —Cl —CH₃ GPP O —Cl —F —F GPQ O —Cl —F —Cl GPR O —Cl —F—CH₃

4.1 Definitions

As used herein, the terms used above having following meaning:

“—(C₁-C₁₀)alkyl” means a straight chain or branched non-cyclichydrocarbon having from 1 to 10 carbon atoms. Representative straightchain —(C₁-C₁₀)alkyls include -methyl, -ethyl, -n-propyl, -n-butyl,-n-pentyl, -n-hexyl, -n-heptyl, -n-octyl, -n-nonyl, and -n-decyl.Representative branched —(C₁-C₁₀)alkyls include -isopropyl, -sec-butyl,-isobutyl, -tert-butyl, -isopentyl, -neopentyl, 1-methylbutyl,2-methylbutyl, 3-methylbutyl, 1,1-dimethylpropyl, 1,2-dimethylpropyl,1-methylpentyl, 2-methylpentyl, 3-methylpentyl, 4-methylpentyl,1-ethylbutyl, 2-ethylbutyl, 3-ethylbutyl, 1,1-dimethylbutyl,1,2-dimethylbutyl, 1,3-dimethylbutyl, 2,2-dimethylbutyl,2,3-dimethylbutyl, 3,3-dimethylbutyl, 1-methylhexyl, 2-methylhexyl,3-methylhexyl, 4-methylhexyl, 5-methylhexyl,1,2-dimethylpentyl,-1,3-dimethylpentyl, 1,2-dimethylhexyl,1,3-dimethylhexyl, 3,3-dimethylhexyl, 1,2-dimethylheptyl,1,3-dimethylheptyl, and 3,3-dimethylheptyl.

“—(C₁-C₆)alkyl” means a straight chain or branched non-cyclichydrocarbon having from 1 to 6 carbon atoms. Representative straightchain —(C₁-C₆)alkyls include -methyl, -ethyl, -n-propyl, -n-butyl,-n-pentyl, and -n-hexyl. Representative branched —(C₁-C₆)alkyls include-isopropyl, -sec-butyl, -isobutyl, -tert-butyl, -isopentyl, -neopentyl,1-methylbutyl, 2-methylbutyl, 3-methylbutyl, 1,1-dimethylpropyl,1,2-dimethylpropyl, 1-methylpentyl, 2-methylpentyl, 3-methylpentyl,4-methylpentyl, 1-ethylbutyl, 2-ethylbutyl, 3-ethylbutyl,1,1-dimethtylbutyl, 1,2-dimethylbutyl, 1,3-dimethylbutyl,2,2-dimethylbutyl, 2,3-dimethylbutyl, and 3,3-dimethylbutyl.

“—(C₁-C₄)alkyl” means a straight chain or branched non-cyclichydrocarbon having from 1 to 4 carbon atoms. Representative straightchain —(C₁-C₄)alkyls include -methyl, -ethyl, -n-propyl, and -n-butyl.Representative branched —(C₁-C₄)alkyls include -isopropyl, -sec-butyl,-isobutyl, and -tert-butyl.

“—(C₂-C₁₀)alkenyl” means a straight chain or branched non-cyclichydrocarbon having from 2 to 10 carbon atoms and including at least onecarbon-carbon double bond. Representative straight chain and branched(C₂-C₁₀)alkenyls include -vinyl, -allyl, -1-butenyl, -2-butenyl,-isobutylenyl, -1-pentenyl, -2-pentenyl, -3-methyl-1-butenyl,-2-methyl-2-butenyl, -2,3-dimethyl-2-butenyl, -1-hexenyl, -2-hexenyl,-3-hexenyl, -1-heptenyl, -2-heptenyl, -3-heptenyl, -1-octenyl,-2-octenyl, -3-octenyl, -1-nonenyl, -2-nonenyl, -3-nonenyl, -1-decenyl,-2-decenyl, -3-decenyl and the like.

“—(C₂-C₆)alkenyl” means a straight chain or branched non-cyclichydrocarbon having from 2 to 6 carbon atoms and including at least onecarbon-carbon double bond. Representative straight chain and branched(C₂-C₆)alkenyls include -vinyl, -allyl, -1-butenyl, -2-butenyl,-isobutylenyl, -1-pentenyl, -2-pentenyl, -3-methyl-1-butenyl,-2-methyl-2-butenyl, -2,3-dimethyl-2-butenyl, -1-hexenyl, 2-hexenyl,3-hexenyl and the like.

“—(C₂-C₁₀)alkynyl” means a straight chain or branched non-cyclichydrocarbon having from 2 to 10 carbon atoms and including at least onecarbon-carbon triple bond. Representative straight chain and branched—(C₂-C₁₀)alkynyls include -acetylenyl, -propynyl, -1-butynyl,-2-butynyl, -1-pentynyl, -2-pentynyl, -3-methyl-1-butynyl, -4-pentynyl,-1-hexynyl, -2-hexynyl, -5-hexynyl, -1-heptynyl, -2-heptynyl,-6-heptynyl, -1-octynyl, -2-octynyl, -7-octynyl, -1-nonynyl, -2-nonynyl,-8-nonynyl, -1-decynyl, -2-decynyl, -9-decynyl and the like.

“—(C₂-C₆)alkynyl” means a straight chain or branched non-cyclichydrocarbon having from 2 to 6 carbon atoms and including at least onecarbon-carbon triple bond. Representative straight chain and branched(C₂-C₆)alkynyls include -acetylenyl, -propynyl, -1-butynyl, -2-butynyl,-1-pentynyl, -2-pentynyl, -3-methyl-1-butynyl, -4-pentynyl, -1-hexynyl,-2-hexynyl, -5-hexynyl and the like.

“—(C₃-C₁₀)cycloalkyl” means a saturated cyclic hydrocarbon having from 3to 10 carbon atoms. Representative (C₃-C₁₀ )cycloalkyls are-cyclopropyl, -cyclobutyl, -cyclopentyl, -cyclohexyl, -cycloheptyl,-cyclooctyl, -cyclononyl, and -cyclodecyl.

“—(C₃-C₈)cycloalkyl” means a saturated cyclic hydrocarbon having from 3to 8 carbon atoms. Representative (C₃-C₈)cycloalkyls include-cyclopropyl, -cyclobutyl, -cyclopentyl, -cyclohexyl, -cycloheptyl, and-cyclooctyl. “—(C₈-C₁₄)bicycloalkyl” means a bi-cyclic hydrocarbon ringsystem having from 8 to 14 carbon atoms and at least one saturatedcyclic alkyl ring. Representative —(C₈-C₁₄)bicycloalkyls include-indanyl, -1,2,3,4-tetrahydronaphthyl, -5,6,7,8-tetrahydronaphthyl,-perhydronaphthyl, and the like.

“—(C₈-C₁₄)tricycloalkyl” means a tri-cyclic hydrocarbon ring systemhaving from 8 to 14 carbon atoms and at least one saturated ring.Representative —(C₈-C₁₄)tricycloalkyls include -pyrenyl,-1,2,3,4-tetrahydroanthracenyl, -perhydroanthracenyl -aceanthreneyl,-1,2,3,4-tetrahydropenanthrenyl, -5,6,7,8-tetrahydrophenanthrenyl,-perhydrophenanthrenyl and the like.

“—(C₅-C₁₀)cycloalkenyl” means a cyclic non-aromatic hydrocarbon havingat least one carbon-carbon double bond in the cyclic system and from 5to 10 carbon atoms. Representative (C₅-C₁₀)cycloalkenyls include-cyclopentenyl, -cyclopentadienyl, -cyclohexenyl,-cyclohexadienyl,-cycloheptenyl, -cycloheptadienyl, -cycloheptatrienyl,-cyclooctenyl, -cyclooctadienyl, -cyclooctatrienyl, -cyclooctatetraenyl,-cyclononenyl -cyclononadienyl, -cyclodecenyl, -cyclodecadienyl and thelike.

“—(C₅-C₈)cycloalkenyl” means a cyclic non-aromatic hydrocarbon having atleast one carbon-carbon double bond in the cyclic system and from 5 to 8carbon atoms. Representative (C₅-C₈)cycloalkenyls include-cyclopentenyl, -cyclopentadienyl, -cyclohexenyl, -cyclohexadienyl,-cycloheptenyl, -cycloheptadienyl, -cycloheptatrienyl, -cyclooctenyl,-cyclooctadienyl, -cyclooctatrienyl, -cyclooctatetraenyl and the like.

“—(C₈-C₁₄)bicycloalkenyl” means a bi-cyclic hydrocarbon ring systemhaving at least one carbon-carbon double bond in each ring and from 8 to14 carbon atoms. Representative —(C₈-C₁₄)bicycloalkenyls include-indenyl, -pentalenyl, -naphthalenyl, -azulenyl, -heptalenyl,-1,2,7,8-tetrahydronaphthalenyl and the like.

“—(C₈-C₁₄)tricycloalkenyl” means a tri-cyclic hydrocarbon ring systemhaving at least one carbon-carbon double bond in each ring and from 8 to14 carbon atoms. Representative —(C₈-C₁₄)tricycloalkenyls include-anthracenyl, -phenanthrenyl, -phenalenyl, -acenaphthalenyl,as-indacenyl, s-indacenyl and the like.

“-(3-to 7-membered)heterocycle” or “-(3-to 7-membered)heterocyclo” meansa 3-to 7-membered monocyclic heterocyclic ring which is eithersaturated, unsaturated non-aromatic, or aromatic. A 3-membered-heterocycle can contain up to 3 heteroatoms, and a 4-to7-memberedheterocycle can contain up to 4 heteroatoms. Each heteroatomis independently selected from nitrogen, which can be quaternized;oxygen; and sulfur, including sulfoxide and sulfone. The -(3-to7-membered)heterocycle can be attached via a nitrogen or carbon atom.Representative -(3-to 7-membered)heterocycles include pyridyl, furyl,thiophenyl, pyrrolyl, oxazolyl, imidazolyl, thiazolyl, thiadiazolyl,isoxazolyl, pyrazolyl, isothiazolyl, pyridazinyl, pyrimidinyl,pyrazinyl, triazinyl, morpholinyl, pyrrolidinonyl, yrrolidinyl,piperidinyl, piperazinyl, hydantoinyl, valerolactamyl, oxiranyl,oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydropyrindinyl,tetrahydropyrimidinyl, tetrahydrothiophenyl, tetrahydrothiopyranyl andthe like.

“-(3-to 5-membered)heterocycle” or “-(3-to 5-membered)heterocyclo” meansa 3-to 5-membered monocyclic heterocyclic ring which is eithersaturated, unsaturated non-aromatic, or aromatic. A 3-memberedheterocycle can contain up to 3 heteroatoms, and a 4-to 5-memberedheterocycle can contain up to 4 heteroatoms. Each heteroatom isindependently selected from nitrogen, which can be quaternized; oxygen;and sulfur, including sulfoxide and sulfone. The -(3-to5-membered)heterocycle can be attached via a nitrogen or carbon atom.Representative -(3-to 5-membered)heterocycles include furyl, thiophenyl,pyrrolyl, oxazolyl, imidazolyl, thiazolyl, isoxazolyl, pyrazolyl,isothiazolyl, triazinyl, pyrrolidinonyl, pyrrolidinyl, hydantoinyl,oxiranyl, oxetanyl, tetrahydrofuranyl, tetrahydrothiophenyl and thelike.

“-(7-to 10-membered)bicycloheterocycle” or “-(7-to10-membered)bicycloheterocyclo” means a 7-to 10-membered bicyclic,heterocyclic ring which is either saturated, unsaturated non-aromatic,or aromatic. A -(7-to 10-membered)bicycloheterocycle contains from 1 to4 heteroatoms independently selected from nitrogen, which can bequaternized; oxygen; and sulfur, including sulfoxide and sulfone. The-(7-to 10-membered)bicycloheterocycle can be attached via a nitrogen orcarbon atom. Representative -(7-to 10-membered)bicycloheterocyclesinclude -quinolinyl, -isoquinolinyl, -chromonyl, -coumarinyl, -indolyl,-indolizinyl, -benzo[b]furanyl, -benzo[b]thiophenyl, -indazolyl,-purinyl, -4H-quinolizinyl, -isoquinolyl, -quinolyl, -phthalazinyl,-naphthyridinyl, -carbazolyl, -, β-carbolinyl and the like.

“—(C₁₄)aryl” means a 14-membered aromatic carbocyclic moiety suchas-anthryl or -phenanthryl.

“-(5-to 10-membered)heteroaryl” means an aromatic heterocycle ring of 5to 10 members, including both mono-and bicyclic ring systems, wherein atleast one carbon atom of one or both of the rings is replaced with aheteroatom independently selected from nitrogen, oxygen, and sulfur. Oneor both of the -(5-to 10-membered)heteroaryl's rings contain at leastone carbon atom. Representative -(5-to 10-membered)heteroaryls includepyridyl, furyl, benzofuranyl, thiophenyl, benzothiophenyl, quinolinyl,pyrrolyl, indolyl, oxazolyl, benzoxazolyl, imidazolyl, benzimidazolyl,thiazolyl, benzothiazolyl, isoxazolyl, pyrazolyl, isothiazolyl,pyridazinyl, pyrimidinyl, pyrazinyl, thiadiazolyl, triazinyl,cinnolinyl, phthalazinyl, and quinazolinyl.

“—CH₂(halo)” means a methyl group wherein one of the hydrogens of themethyl group has been replaced with a halogen. Representative —CH₂(halo)groups include —CH₂F, —CH₂Cl, —CH₂Br, and —CH₂I.

“—CH(halo)₂” means a methyl group wherein two of the hydrogens of themethyl group have been replaced with a halogen. Representative—CH(halo)₂ groups include —CHF₂, —CHCl₂, —CHBr₂, CHBrCl, CHClI, and—CHI_(2.)

“—C(halo)₃” means a methyl group wherein each of the hydrogens of themethyl group has been replaced with a halogen. Representative —C(halo)₃groups include —CF₃, —CCl₃, —CBr₃, and —CI₃.

“-Halogen” or “-Halo” means —F, —Cl, —Br, or —I.

The phrase “pyridyl group” means

wherein R₁, R₂, and n are defined above for the BenzoazolylpiperazineCompounds of formula (Ia, IIa, and IIIa).

The phrase “pyrazinyl group” means,

wherein R₁, R₂, and p are defined above for the BenzoazolylpiperazineCompounds of formula (Ib, IIa, and IIIb).

The phrase “pyrimidinyl group” means

wherein R₁, R₂, and p are defined above for the BenzoazolylpiperazineCompounds of formula (Ia), (IIa), and (IIIa).

The phrase “pyridazinyl group” means

wherein R₁, R₂, and p are defined above for the BenzoazolylpiperazineCompounds of formula (Ib), (Ilb), and (IIIb).

The phrase “thiazanyl group” means

wherein R₁ is defined above for the Benzoazolylpiperazine Compounds offormula (Ib), (IIb), and (IIIb).

The phrase “2-(3-chloropyridyl)” means

The phrase “2-(3-methylpyridyl)” means

The phrase “2-(3-CF₃-pyridyl)” means

The phrase “2-(3-CHF₂-pyridyl)” means

The phrase “2-(3-hydroxypyridyl)” means

The phrase “2-(3-nitropyridyl)” means

The phrase “2-(3-cyanopyridyl)” means

The phrase “2-(3-bromopyridyl)” means

The phrase “2-(3-iodopyridyl)” means

The phrase “4-(5-chloropyrimidinyl)” means

The phrase “4-(5-methylpyrimidinyl)” means

The phrase “4-(5-fluoropyrimidinyl)” means

The phrase “2-(3-chloropyrazinyl)” means

The phrase “2-(3-methylpyrazinyl)” means

The phrase “2-(3-fluoropyrazinyl)” means

The phrase “3-(4-chloropyridazinyl)” means

The phrase “3-(4-methylpyridazinyl)” means

The phrase “3-(4-fluoropyridazinyl)” means

The phrase “5-(4-chlorothiazanyl)” means

The phrase “5-(4-methylthiazanyl)” means

The phrase “2-pyrazinyl” means

The phrase “2-pyridazinyl” means

The phrase “4-thiazanyl” means

The phrase “5-(4-fluorothiazanyl)” means

The phrase “benzoimidiazolyl group” means

wherein R₈, R₉ and R₁₀ are defined above for the BenzoazolylpiperazineCompounds of formula (IIa) and (IIb).

The phrase “benzothiazolyl group” means

wherein R₈ and R₉ are defined above for the BenzoazolylpiperazineCompounds of formula (Ia) and (Ib).

The phrase “benzooxazolyl group” means

wherein R₈ and R₉ are defined above for the BenzoazolylpiperazineCompounds of formula (IIIa) and (IIIb).

The term “animal,” includes, but is not limited to, a cow, monkey,baboon, chimpanzee, horse, sheep, pig, chicken, turkey, quail, cat, dog,mouse, rat, rabbit, guinea pig, and human.

The phrase “pharmaceutically acceptable salt,” as used herein, includesa salt formed from an acid and a basic nitrogen group of one of theBenzoazolylpiperazine Compounds. Illustrative salts include, but are notlimited, to sulfate, citrate, acetate, oxalate, chloride, bromide,iodide, nitrate, bisulfate, phosphate, acid phosphate, isonicotinate,lactate, salicylate, acid citrate, tartrate, oleate, tannate,pantothenate, bitartrate, ascorbate, succinate, maleate, gentisinate,fumarate, gluconate, glucaronate, saccharate, formate, benzoate,glutamate, methanesulfonate, ethanesulfonate, benzenesulfonate,p-toluenesulfonate, and pamoate (i.e.,1,1′-methylene-bis-(2-hydroxy-3-naphthoate)) salts. The term“pharmaceutically acceptable salt” also includes a salt prepared from aBenzoazolylpiperazine Compound having an acidic finctional group, suchas a carboxylic acid finctional group, and a pharmaceutically acceptableinorganic or organic base. Suitable bases include, but are not limitedto, hydroxides of alkali metals such as sodium, potassium, and lithium;hydroxides of alkaline earth metal such as calcium and magnesium;hydroxides of other metals, such as aluminum and zinc; ammonia andorganic amines, such as unsubstituted or hydroxy-substituted mono-, di-,or trialkylamines; dicyclohexylamine; tributyl amine; pyridine;N-methyl,N-ethylamine; diethylamine; triethylamine; mono-, bis-, ortris-(2-hydroxy-lower alkyl amines), such as mono-, bis-, ortris-(2-hydroxyethyl)amine, 2-hydroxy-tert-butylamine, ortris-(hydroxymethyl)methylamine, N,N,-di-lower alkyl-N-(hydroxy loweralkyl)-amines, such as N,N,-dimethyl-N-(2-hydroxyethyl)amine, ortri-(2-hydroxyethyl)amine; N-methyl-D-glucamine; and amino acids such asarginine, lysine and the like.

The phrase “effective amount,” when used in connection with aBenzoazolylpiperazine Compound means an amount effective for: (a)treating or preventing pain, UI, an ulcer, IBD, IBS, an addictivedisorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke,a seizure, a pruritic condition, psychosis, a cognitive disorder, amemory deficit, restricted brain function, Huntington's chorea, ALS,dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia,or depression; or (b) inhibiting VR1, mGluR1, or mGluR5 function in acell.

The phrase “effective amount,” when used in connection with the anothertherapeutic agent means an amount for providing the therapeutic effectof the therapeutic agent.

When a first group is “substituted with one or more” second groups, oneor more hydrogen atoms of the first group is replaced with acorresponding number of second groups. When the number of second groupsis two or greater, each second group can be the same or different. Inone embodiment, the number of second groups is one or two. In anotherembodiment, the number of second groups is one.

The term “DMSO” means dimethyl sulfoxide.

The term “DCM” means dichloromethane.

The term “UI” means urinary incontinence.

The term “IBD” means inflammatory-bowel disease.

The term “IBS” means irritable-bowel syndrome.

The term “ALS” means amyotrophic lateral sclerosis.

The phrase “treatment of” and “treating” includes the amelioration orcessation of pain, UI, an ulcer, IBD, IBS, an addictive disorder,Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure,a pruritic condition, psychosis, a cognitive disorder, a memory deficit,restricted brain function, Huntington's chorea, ALS, dementia,retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, ordepression, or a symptom thereof.

The phrase “prevention of” and “preventing” includes the avoidance ofthe onset of pain, UI, an ulcer, IBD, IBS, an addictive disorder,Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure,a pruritic condition, psychosis, a cognitive disorder, a memory deficit,restricted brain function, Huntington's chorea, ALS, dementia,retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, ordepression, or a symptom thereof.

4.2 Methods for Making the Benzoazolylpiperazine Compounds

The Benzoazolylpiperazine Compounds can be made using conventionalorganic synthesis or by the following illustrative methods shown in theschemes below.

4.2.1 Methods for Making the Benzoazolypiperazine Compounds of Formula(IA) and (IB) wherein X is 1 and A is —C(O)—NR₄

The Benzoazolylpiperazine Compounds of formula (Ia) and (Ib) wherein xis 1, A is —C(O)—NR₄—, and R₄ is —H, can be obtained by the followingillustrative method shown in Scheme A:

A compound of formula B (about 2 mmol) is dissolved in an aproticorganic solvent (about 3 mL). To the resulting solution is added acompound of formula A (about 2 mmol) and the resulting reaction mixtureallowed to stir for about 10 min. The solvent is then removed underreduced pressure to provide the Benzoazolylpiperazine Compound offormula (Ia) or (Ib) wherein x is 1, A is —(O)—NR₄—, and R₄ is —H. TheBenzoazolylpiperazine Compounds of formula (Ia) and (Ib) can be purifiedon a silica column eluted with 5:95 ethyl acetate/hexane.

The compound of formula B can be obtained as shown below in Scheme B:

A compound of formula D (about 0.75 eq.) in an aprotic organic solvent(about 0.04 M) is cooled to about 0° C. To the cooled solution is slowlyadded a solution of a compound of formula C (about 0.75 eq.) in anaprotic organic solvent (about 0.4 M). The resulting reaction mixture isstirred at 0° C. for about 5 min. and about 0.75 eq. of triethylamineare added to the reaction mixture. The reaction mixture is then allowedto warm to room temperature and the solvent is then removed underreduced pressure to provide the compound of formula B. The compound offormula D is commercially available from Sigma-Aldrich, St. Louis, Mo.(www.sigma-aldrich.com). Compounds of formula C are commerciallyavailable or can be prepared by the following illustrative method shownbelow in Scheme C.

To a stirred solution of aniline U (about 74 mmol) and potassiumthiocyanate (about 148 mmol) in about 100 mL of glacial acetic acid isadded dropwise a solution of bromine (about 74 mmol) in about 25 mL ofglacial acetic acid. The flask containing the bromine in acetic acid isthen rinsed with about 15 mL of acetic acid which is combined with thesolution of aniline U. The resulting reaction mixture is vigorouslystirred at room temperature for between about 2 h and about 24 h. Thereaction mixture is then poured over crushed ice (about 500 mL) and thepH of the resulting mixture adjusted to a value of about 10 usingammonium hydroxide to provide a precipitate. The resulting precipitateis collected by filtration and recrystallized from toluene to providethe compound of formula C. Compounds of formula U are commerciallyavailable or can be prepared by methods well known to those skilled inthe art.

The compound of formula A can be obtained as shown below in Scheme D:

A compound of formula F1-F5 (about 20 mmol) is reacted with a compoundof formula E (about 27.5 mmol) in about 15 mL of DMSO in the presence oftriethylamine (about 30 mmol), optionally with heating, for about 24 hto provide a compound of formula A. The compound of formula A isisolated from the reaction mixture and purified. In one embodiment, thecompound of formula A is purified using column chromatography orrecrystallization.

Compounds of formula E and F are commercially available or can beprepared by methods well known to those skilled in the art. The compoundof formula E wherein m is 0 and the compound of formula E wherein m is 1and R₃ is (R) —CH₃ or (S) —CH₃ are commercially available fromSigma-Aldrich, St. Louis, Mo. (www.sigma-aldrich.com). In oneembodiment, X is bromide, chloride, or iodide.

The Benzoazolylpiperazine Compounds of formula (Ia) and (Ib) wherein xis 1, A is —(O)—NR₄—, and R₄ is —(C₁-C₆)alkyl can be obtained by thefollowing illustrative method shown below in Scheme E.

To a solution of a Benzoazolylpiperazine compound of formula (Ia) or(Ib) wherein x is 1, A is —C(O)—NR₄—, and R₄ is —H (about 1 eq.),obtained as described above in Scheme A, in DMF at 0° C., is added a DMFsolution of NaH (about 2 eq.). The resulting reaction mixture is allowedto warm to room temperature over about 1 h. To the resulting mixture isadded about 1.2 eq. of an alkyl halide, R₄X, and the resulting reactionmixture allowed to stir until the Benzoazolylpiperazine Compounds offormula (Ia) and (Ib) wherein x is 1, A is —C(O)—NR₄—, and R₄ is—(C₁-₆)alkyl is formed. The progress of the reaction can be monitoredusing conventional analytical techniques including, but not limited to,high pressure liquid chromatography (HPLC), column chromatography,thin-layer chromatography (TLC), column chromatography, gaschromatography, mass spectrometry, and nuclear magnetic resonancespectroscopy such as ¹H and ¹³C NMR. The Benzoazolylpiperazine Compoundsof formula (Ia) and (Ib) wherein x is 1, A is —C(O)—NR₄—, and R₄ is—(C₁-C₆)alkyl is then isolated and purified. In one embodiment, theBenzoazolylpiperazine Compounds of formula (Ia) and (Ib) wherein x is 1,A is —C(O)—NR₄—, and R₄ is —(C₁-C₆)alkyl is isolated by removing thesolvent under reduced pressure. In another embodiment, theBenzoazolylpiperazine Compounds of formula (Ia) and (Ib) wherein x is 1,A is —C(O)—NR₄—, and R₄ is —(C₁-C₆)alkyl is isolated by extraction. TheBenzoazolylpiperazine Compounds of formula (Ia) and (Ib) wherein x is 1,A is —C(O)—NR₄—, and R₄ is —(C₁-C₆)alkyl can be purified, for example,by column chromatography or recrystallization.

4.2.2 Methods for Making the Benzoazolypiperazine Compounds of Formula(IA) and (IB) wherein X is 1 and A is —(S)—NR₄

The Benzoazolylpiperazine Compounds of formula (Ia) and (Ib) wherein xis 1, A is —C(S)—NR₄—, and R₄ is —H can be obtained by the followingillustrative method in Scheme F:

A Compound of Formula C (about 2 mmol), 1,1′-thiocarbonyldiimidazole(about 2 mmol) (commercially available from Sigma-Aldrich, St. Louis,Mo. (www.sigma-aldrich.com)), and 4-dimethylaminopyridine (DMAP)(commercially available from Sigma-Aldrich, St. Louis, Mo.(www.sigma-aldrich.com)) are suspended in DMSO (about 3 mL) at roomtemperature and the resulting mixture is heated at about 100° C. forabout 6 h. The resulting reaction mixture is then cooled to roomtemperature and a compound of Formula A (about 2 mmol) is added to thereaction mixture and the reaction mixture is heated to about 100° C. forabout 16 h. The solvent is then removed under reduced pressure toprovide the Benzoazolylpiperazine Compound of formula (Ia) or (Ib)wherein x is 1, A is —C(S)—NR₄—, and R₄ is —H. The BenzoazolylpiperazineCompounds of formula (Ia) and (Ib) can be purified on a silica columneluted with 5:95 ethyl acetate/hexane.

The Benzoazolylpiperazine Compounds of formula (Ia) and (Ib) wherein xis 1, A is —C(S)—NR₄—, and R₄ is —(C₁-C₆)alkyl can be obtained by amethod analogous to the method used to obtain the BenzoazolylpiperazineCompounds of formula (Ia) and (Ib) wherein x is 1, A is —C(O)—NR₄—, andR₄ is —(C₁-C₆)alkyl as described in Scheme E except that aBenzoazolylpiperazine Compound of formula (Ia) and (Ib) wherein x is 1,A is —(S)—NR₄—, and R₄ is —H, obtained as described above in Scheme F,is used in place of the Benzoazolylpiperazine Compounds of formula (Ia)and (Ib) wherein x is 1, A is —C(O)—NR₄—, and R₄ is —H.

4.2.3 Methods for Making the Benzoazolylpiperazine Compounds of Formula(IA) and (IB) wherein X is 0

The Benzoazolylpiperazine Compounds of formula (Ia) and (Ib) wherein xis 0 can be obtained by the following illustrative method shown below inScheme G:

A compound of Formula A (about 1 mmol) and a compound of Formula G(about 1 mmol) are dissolved in DMSO (about 3 mL) and heated at atemperature of between about 140° C. and 150° C. for about 12 h. Themixture is cooled to room temperature and the solvent removed underreduced pressure to provide a residue that is purified using silica gelflash chromatography (gradient elution from 2:98 methanol:DCM to 6:94methanol:DCM) to provide the Benzoazolylpiperazine Compound of formula(Ia) or (Ib) wherein x is 0.

The compound of Formula A can be obtained as shown above in Scheme D.

The compounds of Formula G are commercially available or can be preparedby procedures well known to those skilled in the art. An illustrativemethod for preparing compounds of Formula G is shown below in Scheme H.

A compound of Formula Z (about 5 to about 10 mmol) and carbodiimidazole(CDI) (commercially available from Sigma-Aldrich, St. Louis, Mo.(www.sigma-aldrich.com)) (about 2 eq) is dissolved in THF (about 50 toabout 70 mL) and the resulting reaction mixture is heated at refluxtemperature for about 4 hours. The reaction mixture is then concentratedunder reduced pressure to provide a residue. Ethyl acetate (about 50 mL)is added to the residue and the resulting insoluble material iscollected by filtration and washed with ethyl acetate to provide acompound of Formula AA. The compound of Formula AA is then reacted withPOCl₃ according to the procedure described in J. Med. Chem. 40:586-593(1997) to provide the compound of Formula BB. The compounds of Formula Zare commercially available or can be prepared by procedures well knownto those skilled in the art. An illustrative procedure for obtaining acompound of Formula Z is shown below in Scheme I:

Thiol CC (about 12 mmol) is dissolved in concentrated sulfuric acid(about 10 mL) at 0° C. and the resulting solution cooled to atemperature of about −13° C. to about −15° C. About 1 mL of 70% nitricacid is added to the resulting solution over a time period of about 30min. and the resulting reaction mixture allowed to stir for about 2 h ata temperature of between about −13° C. to about −15° C. The reactionmixture is then poured into ice water (about 100 mL), neutralized with5% to 10% aqueous sodium hydroxide, and extracted with about 50 mL ofchloroform. The chloroform layer is separated from the aqueous layer andremoved under reduced pressure to provide a residue that is purifiedusing flash chromatography (silica column and chloroform eluant) toprovide a compound of Formula DD. The compound of Formula DD isdissolved in ethanol (about 50 mL) and hydrogenated for about 12 h atroom temperature using 10% palladium on carbon as a catalyst. Thecatalyst is removed by filtration and the ethanol is removed underreduced pressure to provide a residue that is purified using flashchromatography (silica gel eluted with 20:1 dichloromethane:methanol) toprovide the compound of Formula EE. The compounds of Formula CC arecommercially available or can be prepared by procedures well known tothose skilled in the art.

4.2.4 Methods for Making the Benzoazolylpiperazine Compounds of Formula(IIA) and (IIB) wherein X is 0

The Benzoazolylpiperazine Compounds of formula (IIa) wherein R₁₀ is —Hand formula (IIb) wherein x is 0 and R₁₀ is —H can be obtained by amethod analogous to that used to obtain the BenzoazolylpiperazineCompounds of formula (Ia) and (Ib) wherein x is 0 as described above insection 4.2.3, Scheme G except that a compound of Formula H, shownbelow,

wherein R₈ and R₉ are defined above for the BenzoazolylpiperazineCompounds of formula (IIa) and (IIb), is used in place of the compoundof Formula G as illustrated below in Scheme

A compound of Formula A (about 1 mmol) and a compound of Formula H(about 1 mmol) are dissolved in toluene or p-xylene in a sealed tube andheated at a temperature of between about 140° C. and 150° C. for about 3days. The mixture is cooled to room temperature and the solvent removedunder reduced pressure to provide a residue that is purified using flashchromatography (silica gel with a gradient elution from 2%methanol:dichloromethane to 6% methanol:dichloromethane) to provide theBenzoazolylpiperazine Compound of formula (IIa) and formula (IIb)wherein x is 0.

The compound of Formula A can be obtained as shown above in Scheme D.

The compounds of Formula H are commercially available or can be preparedby procedures well known to those skilled in the art. An illustrativemethod for preparing the compound of Formula H is shown below in SchemeK:

A compound of Formula I (about 5 to about 10 mmol) and carbodiimidazole(CDI) (commercially available from Sigma-Aldrich, St. Louis, Mo.(www.sigma-aldrich.com)) (about 2 eq) is dissolved in THF (about 50 toabout 70 mL) and the resulting reaction mixture is heated at refluxtemperature for about 4 hours. The reaction mixture is then concentratedunder reduced pressure to provide a residue. Ethyl acetate (about 50 mL)is added to the residue and the resulting insoluble material iscollected by filtration and washed with ethyl acetate to provide acompound of Formula J. The compound of Formula J is then reacted withPOCl₃ according to the procedure described in J. Med. Chem. 40:586-593(1997) to provide the compound of Formula H. The compounds of Formula Iare commercially available or can be prepared by procedures well knownto those skilled in the art. An illustrative procedure for obtaining acompound of Formula I is shown below in Scheme L:

Aniline hydrochloride V (about 12 mmol) is dissolved in concentratedsulfuric acid (about 10 mL) at 0° C. and the resulting solution cooledto a temperature of about −13° C. to about −15° C. About 1 mL of 70%nitric acid is added to the resulting solution over a time period ofabout 30 min. and the resulting reaction mixture allowed to stir forabout 2 h at a temperature of between about −13° C. to about −15° C. Thereaction mixture is then poured into ice water (about 100 mL),neutralized with 5% to 10% aqueous sodium hydroxide and extracted withabout 50 mL of chloroform. The chloroform is separated from the aqueouslayer and removed under reduced pressure to provide a residue that ispurified using flash chromatography (silica column and chloroformeluant) to provide a compound of Formula W. The compound of Formula W isdissolved in ethanol (about 50 mL) and hydrogenated for about 12 h atroom temperature using 10% palladium on carbon as a catalyst. Thecatalyst is removed by filtration and the ethanol is removed underreduced pressure to provide a residue that is purified using flashchromatography (silica gel eluted with 20:1 dichloromethane:methanol) toprovide the compound of Formula I. The compounds of Formula V arecommercially available or can be prepared by procedures well known tothose skilled in the art.

The Benzoazolylpiperazine Compounds of formula (IIa) wherein R₁₀ is—(C₁-C₄)alkyl and formula (IIb) wherein x is 0 and R₁₀ is —(C₁-C₄)alkylcan be obtained by a method analogous to that used to obtain theBenzoazolylpiperazine Compounds of formula (IIa) and (IIb) wherein x is0 and R₁₀ is —H, as described above in Scheme J, except that a compoundof Formula K, shown below

wherein R₈ and R₉ are defined above for the BenzoazolylpiperazineCompounds of formula (IIa) and (IIb) and R₁₀ is a —(C₁-C₆)alkyl is usedin place of the compound of Formula H. The compound of Formula K can beobtained as described below in Scheme M

NaH (about 2 eq) is added to a solution of a compound of Formula H inDMF at 0° C. and the resulting mixture is allowed to stir and to warm toroom temperature over a period of about one hour. An alkyl halide,R₁₀—X, (about 1.2 eq) is then added to the solution and the resultingreaction mixture allowed to stir until the compound of Formula K isproduced. In one embodiment, the alkyl halide is an alkyl iodide. Theformation of the compound of Formula K can be monitored by analyticalmethods well known to those skilled in the art including, but notlimited to, liquid chromatography, column chromatography, gaschromatography, thin-layer chromatography, mass spectrometry, andnuclear magnetic resonance spectroscopy such as ¹H and ¹³C NMR. Water isthen added to the reaction mixture to produce a precipitate of thecompound of Formula K which is filtered, collected, and dried.

The compound of Formula H can be obtained as described above in SchemeK.

4.2.5 Methods for Making the Benzoazolylpiperazine Compounds of Formula(IIB) wherein X is 1 and A is —C(O)—NR₄

The Benzoazolylpiperazine Compounds of formula (IIb) wherein x is 1, Ais —C(O)—NR₄—, R₄ is —H, and R₁₀ is —H can be obtained by a methodanalogous to that used to obtain the Benzoazolylpiperazine Compounds offormula (Ia) and (Ib) wherein x is 1, A is —C(O)—NR₄—, and R₄ is —H asdescribed above in Scheme A except that a compound of Formula L, shownbelow,

wherein R₈ and R₉ are defined above for the BenzoazolylpiperazineCompounds of formula (IIb), is used in place of the compound of FormulaB.

The Compound of Formula L can be obtained by a method analogous to thatused to obtain the compound of Formula B as described in section 4.2.1,Scheme B, except that a compound of Formula M, shown below,

wherein R₈ and R₉ are defined above for the BenzoazolylpiperazineCompounds of formula (IIb), is used in place of the compound of FormulaC. Compounds of Formula M are commercially available or can be preparedby procedures well known to those skilled in the art. An illustrativeprocedure for obtaining a compound of Formula M is shown below in SchemeN:

A compound of Formula H (about 1 mmol), prepared as described above inScheme K, is dissolved in excess aqueous ammonia in a sealed tube andheated at a temperature of between about 140° C. and 150° C. for about 3days. The mixture is cooled to room temperature and the solvent removedunder reduced pressure to provide a residue. In another embodiment, themixture is cooled to room temperature, extracted with an organicsolvent, the organic phase separated from the aqueous phase, and theorganic solvent removed under reduced pressure to provide a residue. Theresidue is then purified to provide the compound of Formula M. In oneembodiment, the residue is purified by recrystallization. In anotherembodiment, the residue is purified using flash chromatography.

The Benzoazolylpiperazine Compounds of formula (IIb) wherein x is 1, Ais —C(O)—NR₄—, R₄ is —H, and R₁₀ is —(C₁-C₄)alkyl can be obtained by amethod analogous to that used to obtain the BenzoazolylpoperazineCompounds of formula (IIb) wherein x is 1, A is —C(O)—NR₄—, R₄ is —H,and R₁₀ is —H except that a compound of Formula N, shown below,

wherein R₈, R₉, and R₁₀ are defined above for the BenzoazolylpiperazineCompounds of formula (IIb), is used in place of the Compound of FormulaL. The compound of Formula N can be obtained by a method analogous tothat used to obtain the compound of Formula L except that a compound ofFormula O, shown below,

wherein R₈, R₉, and R₁₀ are defined above for the BenzoazolylpiperazineCompounds of formula (IIb), is used in place of the compound of FormulaM. The compound of Formula O can be obtained as shown below in Scheme N:

NaH (about 2 eq) is added to a solution of a compound of Formula M inDMF at 0° C. and the resulting mixture is allowed to stir and to warm toroom temperature over a period of about one hour. An alkyl halide,R₁₀—X, (about 1 eq.) is then added to the solution and the resultingreaction mixture allowed to stir until a mixture of acompound of FormulaO and a compound of Formula X is produced. In one embodiment, the alkylhalide is an alkyl iodide. The formation of the compound of Formula Oand the compound of Formula X can be monitored by analytical methodswell known to those skilled in the art including, but not limited to,those described above. Water is then added to the reaction mixture toproduce a precipitate of the compound of Formula O and the compound ofFormula X which are collected by filtration. The compound of Formula Oand the compound of Formula X are then separated to provide the compoundof Formula O. The compound of Formula O and the compound of Formula Xcan be separated by analytical methods well known to those skilled inthe art including, but not limited to, column chromatography,preparative TLC, preparative HPLC, and preparative GC.

The Benzoazolylpiperazine Compounds of formula (IIb) wherein x is 1, Ais —C(O)—NR₄—, R₄ is —(C₁-C₆)alkyl, and R₁₀ is —H can be obtained by amethod analogous to that used to obtain the BenzoazolylpiperazineCompounds of formula (Ia) and (Ib) wherein x is 1, A is —C(O)—NR₄—, andR₄ is —(C₁-C₆)alkyl as shown above in Scheme E except that theBenzoazolylpiperazine Compounds of formula (IIb) wherein x is 1, A is—C(O)—NR₄—, R₄ is —H, and R₁₀ is —H, prepared as described above, isused in place of the Benzoazolylpiperazine compound of formula (Ia) or(Ib) wherein x is 1, A is —C(O)—NR₄—, and R₄ is —H.

The Benzoazolylpiperazine Compounds of formula (IIb) wherein x is 1, Ais —C(O)—NR₄—, R₄ is —(C₁-C₆)alkyl, and R₁₀ is —(C₁-C₄)alkyl can beobtained by a method analogous to that used to obtain theBenzoazolylpiperazine Compounds of formula (Ia) and (Ib) wherein x is 1,A is —C(O)—NR₄—, and R₄ is —(C₁-C₆)alkyl as shown above in Scheme Eexcept that the Benzoazolylpiperazine Compounds of formula (IIb) whereinx is 1, A is —C(O)—NR₄—, R₄ is —H, and R₁₀ is —(C₁-C₆)alkyl, prepared asdescribed above, is used in place of the Benzoazolylpiperazine compoundof formula (Ia) or (Ib) wherein x is 1, A is —C(O)—NR₄—, and R₄ is —H.

4.2.6 Methods for Making the Benzoazolylpiperazine Compounds of Formula(IIB) wherein X is 1 and A is —(S)—NR₄—

The Benzoazolylpiperazine Compounds of formula (IIb) wherein x is 1, Ais —(S)—NR₄—, R₄ is —H, and R₁₀ is —H can be obtained by a methodanalogous to that used to obtain the Benzoazolylpiperazine Compounds offormula (Ia) and (Ib) wherein x is 1 and A is —C(S)—NR₄—, and R₄ is —Has described above in Scheme F except that a compound of Formula M isused in place of the compound of Formula C. The compound of Formula Mcan be obtained as described above.

The Benzoazolylpiperazine Compounds of formula (IIb) wherein x is 1, Ais —C(S)—NR₄—, R₄ is —H, and R₁₀ is —(C₁-C₄)alkyl can be obtained by amethod analogous to that used to obtain the BenzoazolylpiperazineCompounds of formula (Ia) and (Ib) wherein x is 1, A is —C(S)—NR₄—, andR₄ is —H, as described in section 4.2.2, Scheme F, except that acompound of Formula O is used in place of the compound of Formula C. Thecompound of Formula O can be obtained as described above.

The Benzoazolylpiperazine Compounds of formula (IIb) wherein x is 1, Ais —C(S)—NR₄—, R₄ is —(C₁-C₆)alkyl, and R₁₀ is —H can be obtained by amethod analogous to that used to obtain the BenzoazolylpiperazineCompounds of formula (Ia) and (Ib) wherein x is 1, A is —C(O)—NR₄—, andR₄ is —(C₁-C₆)alkyl as described above in Scheme E except that theBenzoylpiperazine Compound of Formula (IIa) wherein A is —C(S)—NR₄—, R₄is —H, and R₁₀ is —H, prepared as described above, is used in place ofthe Benzoazolylpiperazine Compounds of formula (Ia) and (Ib) wherein xis 1, A is —C(O)—NR₄—, and R₄ is —H.

The Benzoazolylpiperazine Compounds of formula (IIb) wherein x is 1, Ais —C(S)—NR₄—, R₄ is —(C₁-C₆)alkyl, and R₁₀ is —(C₁-C₄)alkyl can beobtained by a method analogous to that used to obtain theBenzoazolylpiperazine Compounds of formula (Ia) and (Ib) wherein x is 1,A is —C(O)—NR₄—, and R₄ is —(C₁-C₆)alkyl as described above in Scheme Eexcept that the Benzoylpiperazine Compound of Formula (IIa) wherein A is—C(S)—NR₄—, R₄ is —H, and R₁₀ is —(C₁-C₄)alkyl, prepared as describedabove, is used in place of the Benzoazolylpiperazine Compounds offormula (Ia) and (Ib) wherein x is 1, A is —C(O)—NR₄—, and R₄ is —H.

4.2.7 Methods for Making the Benzoazolylpiperazine Compounds of Formula(IIIA) and (IIIB) wherein X is 1 and A is —C(O)—NR₄

The Benzoazolylpiperazine Compounds of formula (IIIa) and (IIIb) whereinx is 1, A is —C(O)—NR₄—, and R₄ is —H can be obtained by a methodanalogous to that used to obtain the Benzoazolylpiperazine Compounds offormula (Ia) and (Ib) wherein x is 1 and A is —C(O)—NR₄ as described insection 4.2.1, Scheme A, except that a compound of Formula P, shownbelow,

wherein R₈ and R₉ are defined above for the BenzoazolylpiperazineCompounds of formula (IIIa) and (IIIb), is used in place of the compoundof Formula B.

The Compound of Formula P can be obtained by a method analogous to thatused to obtain the compound of Formula B as described above in Scheme Bexcept that a compound of Formula Q, shown below,

wherein R₈ and R₉ are defined above for the BenzoazolylpiperazineCompounds of formula (IIIa) and (IIIb), is used in place of the compoundof Formula C. The compounds of Formula Q are commercially available orcan be prepared by procedures well known to those skilled in the art.The compounds of Formula Q can be obtained by a method analogous to thatused to obtain the compound of Formula BB, as described in Scheme H,except that a compound of Formula HH, shown below,

is used in place of a compound of Formula Z.

An illustrative procedure for obtaining a compound of Formula HH isshown below in Scheme O:

Phenol FF (about 12 mmol) is dissolved in concentrated sulfuric acid(about 10 mL) at 0° C. and the resulting solution cooled to atemperature of about −13° C. to about −15° C. About 1 mL of 70% nitricacid is added to the resulting solution over a time period of about 30min. and the resulting reaction mixture allowed to stir for about 2 h ata temperature of between about −13° C. to about −15° C. The reactionmixture is then poured into ice water (about 100 mL), neutralized with5% to 10% aqueous sodium hydroxide, and extracted with about 50 mL ofchloroform. The chloroform is separated from the aqueous layer andremoved under reduced pressure to provide a residue that is purifiedusing flash chromatography (silica column and chloroform eluant) toprovide a compound of Formula GG The compound of Formula GG is dissolvedin ethanol (about 50 mL) and hydrogenated for about 12 h at roomtemperature using 10% palladium on carbon as a catalyst. The catalyst isremoved by filtration and the ethanol is removed under reduced pressureto provide a residue that is purified using flash chromatography (silicagel eluted with 20:1 dichloromethane:methanol) to provide the compoundof Formula HH The compounds of 30 Formula FF are commercially availableor can be prepared by procedures well known to those skilled in the art.

The Benzoazolylpiperazine Compounds of formula (IIIa) and (IIIb) whereinx is 1, A is —C(O)—NR₄—, and R₄ is —(C₁-C₆)alkyl can be obtained by amethod analogous to the method used to obtain the BenzoazolylpiperazineCompounds of formula (Ia) and (Ib) wherein x is 1, A is —C(O)—NR₄—, andR₄ is —(C₁-C₆)alkyl as shown above in Scheme E except that theBenzoazolylpiperazine Compounds of formula (Ia) and (Ib) wherein x is 1,A is —C(O)—NR₄—, and R₄ is —H is replaced with a BenzoazolylpiperazineCompounds of formula (IIIa) and (IIIb) wherein x is 1, A is —C(O)—NR₄—,and R₄ is —H, obtained as described above.

4.2.8 Methods for Making the Benzoazolylpiperazine Compounds of Formula(IIIA) and (IIIB) wherein X is 1 and A is —C(S)—NR₄

The Benzoazolylpiperazine Compounds of formula (IIIa) and (IIIb) whereinx is 1, A is —C(S)—NR₄—, and R₄ is —H can be obtained by a methodanalogous to that used to obtain the Benzoazolylpiperazine Compounds offormula (Ia) and (Ib) wherein x is 1 and A is —C(S)—NR₄—, and R₄ is —Has described above in Scheme F except that a compound of Formula Q isused in place of the compound of Formula C. The compound of Formula Qcan be obtained as described above.

The Benzoazolylpiperazine Compounds of formula (IIIa) and (IIIb) whereinx is 1, A is —C(S)—NR₄—, and R₄ is —(C₁-C₆)alkyl can be obtained by amethod analogous to the method used to obtain the BenzoazolylpiperazineCompounds of formula (Ia) and (Ib) wherein x is 1, A is —C(O)—NR₄—, andR₄ is —(C₁-C₆)alkyl as described in Scheme E except that aBenzoazolylpiperazine Compound of formula (IIIa) and (IIIb) wherein x is1, A is —(S)—NR₄—, and R₄ is —H, obtained as described above, is used inplace of the Benzoazolylpiperazine Compounds of formula (Ia) and (Ib)wherein x is 1, A is —C(O)—NR₄—, and R₄ is —H.

4.2.9 Methods for Making the Benzoazolylpiperazine Compounds of Formula(IIIA) and (IIIB) wherein X is 0

The Benzoazolylpiperazine Compounds of formula (IIIa) and (IIIb) whereinx is 0 can be obtained by the following illustrative method shown inScheme P.

A compound of Formula S (about 15 to about 20 mmol) and a compound ofFormula T (about 1 eq.) are dissolved in ethanol (about 30 to about 40mL) and the resulting reaction mixture heated at reflux temperature forabout 5 h. The reaction mixture is concentrated under reduced pressureto provide a residue that is diluted with water (about 30 mL) andacidified with acetic acid to a pH value of about 6. The aqueous mixtureis then extracted with ethyl acetate, the ethyl acetate dried (Na₂SO₄),and the solvent removed under reduced pressure to provide a compound ofFormula Y which is used without further purification. The compound ofFormula Y (about 1 mmol) and a compound of Formula A (about 1 eq.) aredissolved in toluene or p-xylene (about 0.5. mL to about 1 mL) and thereaction mixture heated in a sealed tube at a temperature of about 150°C. for about 24 h. The reaction mixture is concentrated under reducedpressure to provide a residue. The resulting residue can be purifiedusing flash chromatography (silica gel, 5:95 methanol:DCM) to providethe Benzoazolylpiperazine Compounds of formula (IIIa) and (IIIb) whereinx is 0.

The compounds of Formula S are commercially available or can be preparedby procedures well known to those skilled in the art. An illustrativeprocedure for obtaining a compound of Formula S is shown below in SchemeQ:

Phenol II (about 12 mmol) is dissolved in concentrated sulfiric acid(about 10 mL) at 0° C. and the resulting solution cooled to atemperature of about −13° C. to about −15° C. About 1 mL of 70% nitricacid is added to the resulting solution over a time period of about 30min. and the resulting reaction mixture allowed to stir for about 2 h ata temperature of between about −13° C. to about −15° C. The reactionmixture is then poured into ice water (about 100 mL), neutralized with5% to 10% aqueous sodium hydroxide and extracted with about 50 mL ofchloroform. The chloroform is separated from the aqueous layer andremoved under reduced pressure to provide a residue that is purifiedusing flash chromatography (silica column and chloroform eluant) toprovide a compound of Formula JJ. The compound of Formula JJ isdissolved in ethanol (about 50 mL) and hydrogenated for about 12 h atroom temperature using 10% palladium on carbon as a catalyst. Thecatalyst is removed by filtration and the ethanol is removed underreduced pressure to provide a residue that is purified using flashchromatography (silica gel eluted with 20:1 dichloromethane:methanol) toprovide the compound of Formula S. The compounds of Formula S arecommercially available or can be prepared by procedures well known tothose skilled in the art.

The compound of Formula T is commercially available from Sigma-Aldrich,St. Louis, Mo. (www.sigma-aldrich.com).

The compounds of Formula A can be obtained as described above.

Suitable aprotic organic solvents for use in the illustrative methodsinclude, but are not limited to, DCM, DMSO, chloroform, toluene,benzene, acetonitrile, carbon tetrachloride, pentane, hexane, ligroin,and diethylether. In one embodiment, the aprotic organic solvent is DCM.

Certain Benzoazolylpiperazine Compounds can have one or more asymmetriccenters and therefore exist in different enantiomeric and diastereomericforms. A Benzoazolylpiperazine Compound can be in the form of an opticalisomer or a diastereomer. Accordingly, the invention encompassesBenzoazolylpiperazine Compounds and their uses as described herein inthe form of their optical isomers, diasteriomers, and mixtures thereof,including a racemic mixture.

In addition, one or more hydrogen, carbon or other atoms of aBenzoazolylpiperazine Compound can be replaced by an isotope of thehydrogen, carbon or other atoms. Such compounds, which are encompassedby the present invention, are useful as research and diagnostic tools inmetabolism pharmacokinetic studies and in binding assays.

4.3 Therapeutic Uses of the Benzoazolypiperazine Compounds

In accordance with the invention, the Benzoazolylpiperazine Compoundsare administered to an animal in need of treatment or prevention ofpain, UI, an ulcer, IBD, 113S, an addictive disorder, Parkinson'sdisease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruriticcondition, psychosis, a cognitive disorder, a memory deficit, restrictedbrain function, Huntington's chorea, ALS, dementia, retinopathy, amuscle spasm, a migraine, vomiting, dyskinesia, or depression.

In one embodiment, an effective amount of a BenzoazolylpiperazineCompound can be used to treat or prevent any condition treatable orpreventable by inhibiting VR1. Examples of conditions that are treatableor preventable by inhibiting VR1 include, but are not limited to, pain,UI, an ulcer, IBD, and IBS.

In another embodiment, an effective amount of a BenzoazolylpiperazineCompound can be used to treat or prevent any condition treatable orpreventable by inhibiting mGluR5. Examples of conditions that aretreatable or preventable by inhibiting mGluR5 include, but are notlimited to, pain, an addictive disorder, Parkinson's disease,parkinsonism, anxiety, a pruritic condition, and psychosis.

In another embodiment, an effective amount of a BenzoazolylpiperazineCompound can be used to treat or prevent any condition treatable orpreventable by inhibiting mGluR1. Examples of conditions that aretreatable or preventable by inhibiting mGluR1 include, but are notlimited to, pain, UI, an addictive disorder, Parkinson's disease,parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruriticcondition, psychosis, a cognitive disorder, a memory deficit, restrictedbrain function, Huntington's chorea, ALS, dementia, retinopathy, amuscle spasm, a migraine, vomiting, dyskinesia, and depression.

The Benzoazolylpiperazine Compounds can be used to treat or preventacute or chronic pain. Examples of pain treatable or preventable usingthe Benzoazolylpiperazine Compounds include, but are not limited to,cancer pain, central pain, labor pain, myocardial infarction pain,pancreatic pain, colic pain, post-operative pain, headache pain, musclepain, pain associated with intensive care, arthritic pain, and painassociated with a periodontal disease, including gingivitis andperiodontitis.

The pain to be treated or prevented can be associated with inflammationassociated with an inflammatory disease, which can arise where there isan inflammation of the body tissue, and which can be a localinflammatory response and/or a systemic inflammation. For example, theBenzoazolylpiperazine Compounds can be used to treat, or prevent painassociated with inflammatory disease including, but not limited to:organ transplant rejection; reoxygenation injury resulting from organtransplantation (see Grupp et al., J. Mol, Cell Cardiol. 31:297-303(1999)) including, but not limited to, transplantation of the heart,lung, liver, or kidney; chronic inflammatory diseases of the joints,including arthritis, rheumatoid arthritis, osteoarthritis and bonediseases associated with increased bone resorption; inflammatory boweldiseases, such as ileitis, ulcerative colitis, Barrett's syndrome, andCrohn's disease; inflammatory lung diseases, such as asthma, adultrespiratory distress syndrome, and chronic obstructive airway disease;inflammatory diseases of the eye, including corneal dystrophy, trachoma,onchocerciasis, uveitis, sympathetic ophthalmitis and endophthalmitis;chronic inflammatory disease of the gum, including gingivitis andperiodontitis; tuberculosis; leprosy; inflammatory diseases of thekidney, including uremic complications, glomerulonephritis andnephrosis; inflammatory disease of the skin, including sclerodermatitis,psoriasis and eczema; inflammatory diseases of the central nervoussystem, including chronic demyelinating diseases of the nervous system,multiple sclerosis, AIDS-related neurodegeneration and Alzheimer'sdisease, infectious meningitis, encephalomyelitis, Parkinson's disease,Huntington's disease, amyotrophic lateral sclerosis and viral orautoimmune encephalitis; autoimmune diseases, including Type I and TypeII diabetes mellitus; diabetic complications, including, but not limitedto, diabetic cataract, glaucoma, retinopathy, nephropathy (such asmicroaluminuria and progressive diabetic nephropathy), polyneuropathy,mononeuropathies, autonomic neuropathy, gangrene of the feet,atherosclerotic coronary arterial disease, peripheral arterial disease,nonketotic hyperglycemic-hyperosmolar coma, foot ulcers, joint problems,and a skin or mucous membrane complication (such as an infection, a shinspot, a candidal infection or necrobiosis lipoidica diabeticorum);immune-complex vasculitis, and systemic lupus erythematosus (SLE);inflammatory disease of the heart, such as cardiomyopathy, ischemicheart disease hypercholesterolemia, and artherosclerosis; as well asvarious other diseases that can have significant inflammatorycomponents, including preeclampsia, chronic liver failure, brain andspinal cord trauma, and cancer. The Benzoazolylpiperazine Compounds canalso be used for inhibiting, treating, or preventing pain associatedwith inflammatory disease that can, for example, be a systemicinflammation of the body, exemplified by gram-positive or gram negativeshock, hemorrhagic or anaphylactic shock, or shock induced by cancerchemotherapy in response to pro-inflammatory cytokines, e.g., shockassociated with pro-inflammatory cytokines. Such shock can be induced,e.g., by a chemotherapeutic agent that is administered as a treatmentfor cancer.

The Benzoazolylpiperazine Compounds can be used to treat or prevent UI.Examples of UI treatable or preventable using the BenzoazolylpiperazineCompounds include, but are not limited to, urge incontinence, stressincontinence, overflow incontinence, neurogenic incontinence, and totalincontinence.

The Benzoazolylpiperazine Compounds can be used to treat or prevent anulcer. Examples of ulcers treatable or preventable using theBenzoazolylpiperazine Compounds include, but are not limited to, aduodenal ulcer, a gastric ulcer, a marginal ulcer, an esophageal ulcer,or a stress ulcer.

The Benzoazolylpiperazine Compounds can be used to treat or prevent IBD,including Crohn's disease and ulcerative colitis.

The Benzoazolylpiperazine Compounds can be used to treat or prevent IBS.Examples of IBS treatable or preventable using the BenzoazolylpiperazineCompounds include, but are not limited to, spastic-colon-type IBS andconstipation-predominant IBS.

The Benzoazolylpiperazine Compounds can be used to treat or prevent anaddictive disorder, including but not limited to, an eating disorder, animpulse-control disorder, an alcohol-related disorder, anicotine-related disorder, an amphetamine-related disorder, acannabis-related disorder, a cocaine-related disorder, anhallucinogen-related disorder, an inhalant-related disorders, and anopioid-related disorder, all of which are further sub-classified aslisted below.

Eating disorders include, but are not limited to, Bulimia Nervosa,Nonpurging Type; Bulimia Nervosa, Purging Type; Anorexia; and EatingDisorder not otherwise specified (NOS).

Impulse control disorders include, but are not limited to, IntermittentExplosive Disorder, Kleptomania, Pyromania, Pathological Gambling,Trichotillomania, and Impulse Control Disorder not otherwise specified(NOS).

Alcohol-related disorders include, but are not limited to,Alcohol-Induced Psychotic Disorder with delusions, Alcohol Abuse,Alcohol Intoxication, Alcohol Withdrawal, Alcohol Intoxication Delirium,Alcohol Withdrawal Delirium, Alcohol-Induced Persisting Dementia,Alcohol-Induced Persisting Amnestic Disorder, Alcohol Dependence,Alcohol-Induced Psychotic Disorder with hallucinations, Alcohol-InducedMood Disorder, Alcohol-Induced Anxiety Disorder, Alcohol-Induced SexualDysfunction, Alcohol-Induced Sleep Disorder, Alcohol-Related Disordernot otherwise specified (NOS), Alcohol Intoxication, and AlcoholWithdrawal.

Nicotine-related disorders include, but are not limited to, NicotineDependence, Nicotine Withdrawal, and Nicotine-Related Disorder nototherwise specified (NOS).

Amphetamine-related disorders include, but are not limited to,Amphetamine Dependence, Amphetamine Abuse, Amphetamine Intoxication,Amphetamine Withdrawal, Amphetamine Intoxication Delirium,Amphetamine-Induced Psychotic Disorder with delusions,Amphetamine-Induced Psychotic Disorders with hallucinations,Amphetamine-Induced Mood Disorder, Amphetamine-Induced Anxiety Disorder,Amphetamine-Induced Sexual Dysfunction, Amphetamine-Induced SleepDisorder, Amphetamine Related Disorder not otherwise specified (NOS),Amphetamine Intoxication, and Amphetamine Withdrawal.

Cannabis-related disorders include, but are not limited to, CannabisDependence, Cannabis Abuse, Cannabis Intoxication, Cannabis IntoxicationDelirium, Cannabis-Induced Psychotic Disorder with delusions,Cannabis-Induced Psychotic Disorder with hallucinations,Cannabis-Induced Anxiety Disorder, Cannabis Related Disorder nototherwise specified (NOS), and Cannabis Intoxication.

Cocaine-related disorders include, but are not limited to, CocaineDependence, Cocaine Abuse, Cocaine Intoxication, Cocaine Withdrawal,Cocaine Intoxication Delirium, Cocaine-Induced Psychotic Disorder withdelusions, Cocaine-Induced Psychotic Disorders with hallucinations,Cocaine-Induced Mood Disorder, Cocaine-Induced Anxiety Disorder,Cocaine-Induced Sexual Dysfunction, Cocaine-Induced Sleep Disorder,Cocaine Related Disorder not otherwise specified (NOS), CocaineIntoxication, and Cocaine Withdrawal.

Hallucinogen-related disorders include, but are not limited to,Hallucinogen Dependence, Hallucinogen Abuse, Hallucinogen Intoxication,Hallucinogen Withdrawal, Hallucinogen Intoxication Delirium,Hallucinogen-Induced Psychotic Disorder with delusions,Hallucinogen-Induced Psychotic Disorders with hallucinations,Hallucinogen-Induced Mood Disorder, Hallucinogen-Induced AnxietyDisorder, Hallucinogen-Induced Sexual Dysfunction, Hallucinogen-InducedSleep Disorder, Hallucinogen Related Disorder not otherwise specified(NOS), Hallucinogen Intoxication, and Hallucinogen Persisting PerceptionDisorder (Flashbacks).

Inhalant-related disorders include, but are not limited to, InhalantDependence, Inhalant Abuse, Inhalant Intoxication, Inhalant IntoxicationDelirium, Inhalant-Induced Psychotic Disorder with delusions,Inhalant-Induced Psychotic Disorder with hallucinations,Inhalant-Induced Anxiety Disorder, Inhalant Related Disorder nototherwise specified (NOS), and Inhalant Intoxication.

Opioid-related disorders include, but are not limited to, OpioidDependence, Opioid Abuse, Opioid Intoxication, Opioid IntoxicationDelirium, Opioid-Induced Psychotic Disorder with delusions,Opioid-Induced Psychotic Disorder with hallucinations, Opioid-InducedAnxiety Disorder, Opioid Related Disorder not otherwise specified (NOS),Opioid Intoxication, and Opioid Withdrawal.

The Benzoazolylpiperazine Compounds can be used to treat or preventParkinson's disease and parkinsonism and the symptoms associated withParkinson's disease and parkinsonism, including but not limited to,bradykinesia, muscular rigidity, resting tremor, and impairment ofpostural balance.

The Benzoazolylpiperazine Compounds can be used to treat or preventgeneralized anxiety or severe anxiety and the symptoms associated withanxiety, including but not limited to, restlessness; tension;tachycardia; dyspnea; depression, including chronic “neurotic”depression; panic disorder; agoraphobia and other specific phobias;eating disorders; and personality disorders.

The Benzoazolylpiperazine Compounds can be used to treat or preventepilepsy, including but not limited to, partial epilepsy, generalizedepilepsy, and the symptoms associated with epilepsy, including but notlimited to, simple partial seizures, jacksonian seizures, complexpartial (psychomotor) seizures, convulsive seizures (grand mal ortonic-clonic seizures), petit mal (absence) seizures, and statusepilepticus.

The Benzoazolylpiperazine Compounds can be used to treat or preventstrokes, including but not limited to, ischemic strokes and hemorrhagicstrokes.

The Benzoazolylpiperazine Compounds can be used to treat or prevent aseizure, including but not limited to, infantile spasms, febrileseizures, and epileptic seizures.

The Benzoazolylpiperazine Compounds can be used to treat or prevent apruritic condition, including but not limited to, pruritus caused by dryskin, scabies, dermatitis, herpetiformis, atopic dermatitis, pruritusvulvae et ani, miliaria, insect bites, pediculosis, contact dermatitis,drug reactions, urticaria, urticarial eruptions of pregnancy, psoriasis,lichen planus, lichen simplex chronicus, exfoliative dermatitis,folliculitis, bullous pemphigoid, or fiberglass dermatitis.

The Benzoazolylpiperazine Compounds can be used to treat or preventpsychosis, including but not limited to, schizophrenia, includingparanoid schizophrenia, hebephrenic or disorganized schizophrenia,catatonic schizophrenia, undifferentiated schizophrenia, negative ordeficit subtype schizophrenia, and non-deficit schizophrenia; adelusional disorder, including erotomanic subtype delusional disorder,grandiose subtype delusional disorder, jealous subtype delusionaldisorder, persecutory subtype delusional disorder, and somatic subtypedelusional disorder; and brief psychosis.

The Benzoazolylpiperazine Compounds can be used to treat or prevent acognitive disorder, including but not limited to, delirium and dementiasuch as multi-infarct dementia, dementia pugilistica, dimentia caused byAIDS, and dementia caused by Alzheimer's disease.

The Benzoazolylpiperazine Compounds can be used to treat or prevent amemory deficiency, including but not limited to, dissociative amnesiaand dissociative fugue.

The Benzoazolylpiperazine Compounds can be used to treat or preventrestricted brain function, including but not limited to, that caused bysurgery or an organ transplant, restricted blood supply to the brain, aspinal cord injury, a head injury, hypoxia, cardiac arrest, orhypoglycemia.

The Benzoazolylpiperazine Compounds can be used to treat or preventHuntington's chorea.

The Benzoazolylpiperazine Compounds can be used to treat or prevent ALS.

The Benzoazolylpiperazine Compounds can be used to treat or preventretinopathy, including but not limited to, arteriosclerotic retinopathy,diabetic arteriosclerotic retinopathy, hypertensive retinopathy,non-proliferative retinopathy, and proliferative retinopathy.

The Benzoazolylpiperazine Compounds can be used to treat or prevent amuscle spasm.

The Benzoazolylpiperazine Compounds can be used to treat or prevent amigraine including, but not limited to, migraine without aura (“commonmigraine”), migraine with aura (“classic migraine”), migraine withoutheadache, basilar migraine, familial hemiplegic migraine, migrainousinfarction, and migraine with prolonged aura.

The Benzoazolylpiperazine Compounds can be used to treat or preventvomiting, including but not limited to, nausea vomiting, dry vomiting(retching), and regurgitation.

The Benzoazolylpiperazine Compounds can be used to treat or preventdyskinesia, including but not limited to, tardive dyskinesia and biliarydyskinesia.

The Benzoazolylpiperazine Compounds can be used to treat or preventdepression, including but not limited to, major depression and bipolardisorder.

Applicants believe that the Benzoazolylpiperazine Compounds areantagonists for VR1.

The invention also relates to methods for inhibiting VR1 function in acell comprising contacting a cell capable of expressing VR1 with aneffective amount of a Benzoazolylpiperazine Compound. This method can beused in vitro, for example, as an assay to select cells that express VR1and, accordingly, are useful as part of an assay to select compoundsuseful for treating or preventing pain, UI, an ulcer, IBD, or IBS. Themethod is also useful for inhibiting VR1 function in a cell in vivo, inan animal, a human in one embodiment, by contacting a cell, in ananimal, with an effective amount of a Benzoazolylpiperazine Compound. Inone embodiment, the method is useful for treating or preventing pain inan animal. In another embodiment, the method is useful for treating orpreventing UI in an animal. In another embodiment, the method is usefulfor treating or preventing an ulcer in an animal. In another embodiment,the method is useful for treating or preventing IBD in an animal. Inanother embodiment, the method is useful for treating or preventing IBSin an animal.

Examples of tissue comprising cells capable of expressing VR1 include,but are not limited to, neuronal, brain, kidney, urothelium, and bladdertissue. Methods for assaying cells that express VR1 are well known inthe art.

Applicants believe that the Benzoazolylpiperazine Compounds areantagonists for mGluR5.

The invention also relates to methods for inhibiting mGluR5 function ina cell comprising contacting a cell capable of expressing mGluR5 with anamount of a Benzoazolylpiperazine Compound effective to inhibit mGluR5function in the cell. This method can be used in vitro, for example, asan assay to select cells that express mGluR5 and, accordingly, areuseful as part of an assay to select compounds useful for treating orpreventing pain, an addictive disorder, Parkinson's disease,parkinsonism, anxiety, a pruritic condition, or psychosis. The method isalso useful for inhibiting mGluR5 function in a cell in vivo, in ananimal, a human in one embodiment, by contacting a cell, in an animal,with an amount of a Benzoazolylpiperazine Compound effective to inhibitmGluR5 function in the cell. In one embodiment, the method is useful fortreating or preventing pain in an animal in need thereof. In anotherembodiment, the method is useful for treating or preventing an addictivedisorder in an animal in need thereof. In another embodiment, the methodis useful for treating or preventing Parkinson's disease in an animal inneed thereof. In another embodiment, the method is useful for treatingor preventing parkinsonism in an animal in need thereof. In anotherembodiment, the method is useful for treating or preventing anxiety inan animal in need thereof In another embodiment, the method is usefulfor treating or preventing a pruritic condition in an animal in needthereof. In another embodiment, the method is useful for treating orpreventing psychosis in an animal in need thereof.

Examples of cells capable of expressing mGluR5 are neuronal and glialcells of the central nervous system, particularly the brain, especiallyin the nucleus accumbens. Methods for assaying cells that express mGluR5are well known in the art.

Applicants believe that the Benzoazolylpiperazine Compounds areantagonists for mGluR1.

The invention also relates to methods for inhibiting mGluR1 function ina cell comprising contacting a cell capable of expressing mGluR1 with anamount of a Benzoazolylpiperazine Compound effective to inhibit mGluR1function in the cell. This method can be used in vitro, for example, asan assay to select cells that express mGluR1 and, accordingly, areuseful as part of an assay to select compounds useful for treating orpreventing pain, UI, an addictive disorder, Parkinson's disease,parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruriticcondition, psychosis, a cognitive disorder, a memory deficit, restrictedbrain function, Huntington's chorea, ALS, dementia, retinopathy, amuscle spasm, a migraine, vomiting, dyskinesia, or depression. Themethod is also useful for inhibiting mGluR1 function in a cell in vivo,in an animal, a human in one embodiment, by contacting a cell, in ananimal, with an amount of a Benzoazolylpiperazine Compound effective toinhibit mGluR1 function in the cell. In one embodiment, the method isuseful for treating or preventing pain in an animal in need thereof. Inanother embodiment, the method is useful for treating or preventing UIin an animal in need thereof. In another embodiment, the method isuseful for treating or preventing an addictive disorder in an animal inneed thereof. In another embodiment, the method is useful for treatingor preventing Parkinson's disease in an animal in need thereof. Inanother embodiment, the method is useful for treating or preventingparkinsonism in an animal in need thereof. In another embodiment, themethod is useful for treating or preventing anxiety in an animal in needthereof. In another embodiment, the method is useful for treating orpreventing epilepsy in an animal in need thereof. In another embodiment,the method is useful for treating or preventing stroke in an animal inneed thereof. In another embodiment, the method is useful for treatingor preventing a seizure in an animal in need thereof. In anotherembodiment, the method is useful for treating or preventing a pruriticcondition in an animal in need thereof. In another embodiment, themethod is useful for treating or preventing psychosis in an animal inneed thereof. In another embodiment, the method is useful for treatingor preventing a cognitive disorder in an animal in need thereof Inanother embodiment, the method is useful for treating or preventing amemory deficit in an animal in need thereof. In another embodiment, themethod is useful for treating or preventing restricted brain function inan animal in need thereof. In another embodiment, the method is usefulfor treating or preventing Huntington's chorea in an animal in needthereof. In another embodiment, the method is useful for treating orpreventing ALS in an animal in need thereof In another embodiment, themethod is useful for treating or preventing dementia in an animal inneed thereof. In another embodiment, the method is useful for treatingor preventing retinopathy in an animal in need thereof. In anotherembodiment, the method is useful for treating or preventing a musclespasm in an animal in need thereof. In another embodiment, the method isuseful for treating or preventing a migraine in an animal in needthereof. In another embodiment, the method is useful for treating orpreventing vomiting in an animal in need thereof. In another embodiment,the method is useful for treating or preventing dyskinesia in an animalin need thereof. In another embodiment, the method is useful fortreating or preventing depression in an animal in need thereof.

Examples of cells capable of expressing mGluR1 include, but are notlimited to, cerebellar Purkinje neuron cells, Purkinje cell bodies(punctate), cells of spine(s) of the cerebellum; neurons and neurophilcells of olfactory-bulb glomeruli; cells of the superficial layer of thecerebral cortex; hippocampus cells; thalamus cells; superior colliculuscells; and spinal trigeminal nucleus cells. Methods for assaying cellsthat express mGluR1 are well known in the art.

4.3.1 Therapeutic/Prophylactic Administration and Compositions of theInvention

Due to their activity, the Benzoazolylpiperazine Compounds areadvantageously useful in veterinary and human medicine. As describedabove, the Benzoazolylpiperazine Compounds are useful for treating orpreventing pain, UI, an ulcer, IBD, IBS, an addictive disorder,Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure,a pruritic condition, psychosis, a cognitive disorder, a memory deficit,restricted brain function, Huntington's chorea, ALS, dementia,retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, ordepression in an animal in need thereof.

When administered to an animal, the Benzoazolylpiperazine Compounds canbe administered as a component of a composition that comprises apharmaceutically acceptable vehicle. The present compositions, whichcomprise a Benzoazolylpiperazine Compound, can be administered orally.The Benzoazolylpiperazine Compounds of the invention can also beadministered by any other convenient route, for example, by infusion orbolus injection, by absorption through epithelial or mucocutaneouslinings (e.g., oral, rectal, and intestinal mucosa, etc.) and can beadministered together with another biologically active agent.Administration can be systemic or local. Various delivery systems areknown, e.g., encapsulation in liposomes, microparticles, microcapsules,capsules, etc., and can be used to administer the BenzoazolylpiperazineCompound.

Methods of administration include, but are not limited to, intradermal,intramuscular, intraperitoneal, intravenous, subcutaneous, intranasal,epidural, oral, sublingual, intracerebral, intravaginal, transdermal,rectal, by inhalation, or topical, particularly to the ears, nose, eyes,or skin. The mode of administration can be left to the discretion of thepractitioner. In most instances, administration will result in therelease of the Benzoazolylpiperazine Compounds into the bloodstream.

In specific embodiments, it can be desirable to administer theBenzoazolylpiperazine Compounds locally. This can be achieved, forexample, and not by way of limitation, by local infuision duringsurgery, topical application, e.g., in conjunction with a wound dressingafter surgery, by injection, by means of a catheter, by means of asuppository or enema, or by means of an implant, said implant being of aporous, non-porous, or gelatinous material, including membranes, such assialastic membranes, or fibers.

In certain embodiments, it can be desirable to introduce theBenzoazolylpiperazine Compounds into the central nervous system orgastrointestinal tract by any suitable route, includingintraventricular, intrathecal, and epidural injection, and enema.Intraventricular injection can be facilitated by an intraventricularcatheter, for example, attached to a reservoir, such as an Ommayareservoir.

Pulmonary administration can also be employed, e.g., by use of aninhaler or nebulizer, and formulation with an aerosolizing agent, or viaperfusion in a fluorocarbon or synthetic pulmonary surfactant. Incertain embodiments, the Benzoazolylpiperazine Compounds can beformulated as a suppository, with traditional binders and excipientssuch as triglycerides.

In another embodiment, the Benzoazolylpiperazine Compounds can bedelivered in a vesicle, in particular a liposome (see Langer, Science249:1527-1533 (1990) and Treat et al., Liposomes in the Therapy ofInfectious Disease and Cancer 317-327 and 353-365 (1989)).

In yet another embodiment, the Benzoazolylpiperazine Compounds can bedelivered in a controlled-release system or sustained-release system(see, e.g., Goodson, in Medical Applications of Controlled Release,supra, vol. 2, pp. 115-138 (1984)). Other controlled- orsustained-release systems discussed in the review by Langer, Science249:1527-1533 (1990) can be used. In one embodiment, a pump can be used(Langer, Science 249:1527-1533 (1990); Sefton, CRC Crit. Ref. Biomed.Eng. 14:201(1987); Buchwald et al., Surgery 88:507 (1980); and Saudek etal., N. Engl. J. Med. 321:574 (1989)). In another embodiment, polymericmaterials can be used (see Medical Applications of Controlled Release(Langer and Wise eds., 1974); Controlled Drug Bioavailability, DrugProduct Design and Performance (Smolen and Ball eds., 1984); Ranger andPeppas, J. Macromol. Sci. Rev. Macromol. Chem. 23:61 (1983); Levy etal., Science 228:190 (1985); During et al., Ann. Neurol. 25:351 (1989);and Howard et al., J. Neurosurg. 71:105 (1989)). In yet anotherembodiment, a controlled- or sustained-release system can be placed inproximity of a target of the Benzoazolylpiperazine Compounds, e.g., thespinal column, brain, or gastrointestinal tract, thus requiring only afraction of the systemic dose.

In one embodiment, the pharmaceutically acceptable vehicle is anexcipient Such a pharmaceutical excipient can be a liquid, such as wateror an oil, including those of petroleum, animal, vegetable, or syntheticorigin, such as peanut oil, soybean oil, mineral oil, sesame oil and thelike. The pharmaceutical excipients can be saline, gum acacia, gelatin,starch paste, talc, keratin, colloidal silica, urea and the like. Inaddition, auxiliary, stabilizing, thickening, lubricating, and coloringagents can be used. In one embodiment, the pharmaceutically acceptableexcipients are sterile when administered to an animal. Water is aparticularly useful excipient when the Benzoazolylpiperazine Compound isadministered intravenously. Saline solutions and aqueous dextrose andglycerol solutions can also be employed as liquid excipients,particularly for injectable solutions. Suitable pharmaceuticalexcipients also include starch, glucose, lactose, sucrose, gelatin,malt, rice, flour, chalk, silica gel, sodium stearate, glycerolmonostearate, talc, sodium chloride, dried skim milk, glycerol,propylene, glycol, water, ethanol and the like. The presentcompositions, if desired, can also contain minor amounts of wetting oremulsifying agents, or pH buffering agents.

The present compositions can take the form of solutions, suspensions,emulsion, tablets, pills, pellets, capsules, capsules containingliquids, powders, sustained-release formulations, suppositories,emulsions, aerosols, sprays, suspensions, or any other form suitable foruse. In one embodiment, the composition is in the form of a capsule (seee.g., U.S. Pat. No. 5,698,155). Other examples of suitablepharmaceutical excipients are described in Remington's PharmaceuticalSciences 1447-1676 (Alfonso R. Gennaro ed., 19th ed. 1995), incorporatedherein by reference.

In one embodiment, the Benzoazolylpiperazine Compounds are formulated inaccordance with routine procedures as a composition adapted for oraladministration to human beings. Compositions for oral delivery can be inthe form of tablets, lozenges, aqueous or oily suspensions, granules,powders, emulsions, capsules, syrups, or elixirs, for example. Orallyadministered compositions can contain one or more agents, for example,sweetening agents such as fructose, aspartame or saccharin; flavoringagents such as peppermint, oil of wintergreen, or cherry; coloringagents; and preserving agents, to provide a pharmaceutically palatablepreparation. Moreover, where in tablet or pill form, the compositionscan be coated to delay disintegration and absorption in thegastrointestinal tract thereby providing a sustained action over anextended period of time. Selectively permeable membranes surrounding anosmotically active driving compound are also suitable for orallyadministered compositions. In these latter platforms, fluid from theenvironment surrounding the capsule is imbibed by the driving compound,which swells to displace the agent or agent composition through anaperture. These delivery platforms can provide an essentially zero orderdelivery profile as opposed to the spiked profiles of immediate releaseformulations. A time-delay material such as glycerol monostearate orglycerol stearate can also be used. Oral compositions can includestandard excipients such as mannitol, lactose, starch, magnesiumstearate, sodium saccharin, cellulose, and magnesium carbonate. In oneembodiment, the excipients are of pharmaceutical grade.

In another embodiment, the Benzoazolylpiperazine Compounds can beformulated for intravenous administration. Typically, compositions forintravenous administration comprise sterile isotonic aqueous buffer.Where necessary, the compositions can also include a solubilizing agent.Compositions for intravenous administration can optionally include alocal anesthetic such as lignocaine to lessen pain at the site of theinjection. Generally, the ingredients are supplied either separately ormixed together in unit dosage form, for example, as a dry lyophilizedpowder or water free concentrate in a hermetically sealed container suchas an ampule or sachette indicating the quantity of active agent. Wherethe Benzoazolylpiperazine Compounds are to be administered by infusion,they can be dispensed, for example, with an infusion bottle containingsterile pharmaceutical grade water or saline. Where theBenzoazolylpiperazine Compounds are administered by injection, an ampuleof sterile water for injection or saline can be provided so that theingredients can be mixed prior to administration.

The Benzoazolylpiperazine Compounds can be administered bycontrolled-release or sustained-release means or by delivery devicesthat are well known to those of ordinary skill in the art. Examplesinclude, but are not limited to, those described in U.S. Pat. Nos.3,845,770; 3,916,899; 3,536,809; 3,598,123; 4,008,719; 5,674,533;5,059,595; 5,591,767; 5,120,548; 5,073,543; 5,639,476; 5,354,556; and5,733,566, each of which is incorporated herein by reference. Suchdosage forms can be used to provide controlled- or sustained-release ofone or more active ingredients using, for example, hydropropylmethylcellulose, other polymer matrices, gels, permeable membranes, osmoticsystems, multilayer coatings, microparticles, liposomes, microspheres,or a combination thereof to provide the desired release profile invarying proportions. Suitable controlled- or sustained-releaseformulations known to those of ordinary skill in the art, includingthose described herein, can be readily selected for use with the activeingredients of the invention. The invention thus encompasses single unitdosage forms suitable for oral administration such as, but not limitedto, tablets, capsules, gelcaps, and caplets that are adapted forcontrolled- or sustained-release.

Controlled- or sustained-release pharmaceutical compositions can have acommon goal of improving drug therapy over that achieved by theirnon-controlled or non-sustained counterparts. In one embodiment, acontrolled- or sustained-release composition comprises a minimal amountof a Benzoazolylpiperazine Compound to cure or control the condition ina minimum amount of time. Advantages of controlled- or sustained-releasecompositions include extended activity of the drug, reduced dosagefrequency, and increased patient compliance. In addition, controlled- orsustained-release compositions can favorably affect the time of onset ofaction or other characteristics, such as blood levels of theBenzoazolylpiperazine Compound, and can thus reduce the occurrence ofadverse side effects.

Controlled- or sustained-release compositions can initially release anamount of a Benzoazolylpiperazine Compound that promptly produces thedesired therapeutic or prophylactic effect, and gradually andcontinually release other amounts of the Benzoazolylpiperazine Compoundto maintain this level of therapeutic or prophylactic effect over anextended period of time. To maintain a constant level of theBenzoazolylpiperazine Compound in the body, the BenzoazolylpiperazineCompound can be released from the dosage form at a rate that willreplace the amount of Benzoazolylpiperazine Compound being metabolizedand excreted from the body. Controlled- or sustained-release of anactive ingredient can be stimulated by various conditions, including butnot limited to, changes in pH, changes in temperature, concentration oravailability of enzymes, concentration or availability of water, orother physiological conditions or compounds.

The amount of the Benzoazolylpiperazine Compound that is effective inthe treatment or prevention of pain, UI, an ulcer, IBD, IBS, anaddictive disorder, Parkinson's disease, parkinsonism, anxiety,epilepsy, stroke, a seizure, a pruritic condition, psychosis, acognitive disorder, a memory deficit, restricted brain function,Huntington's chorea, ALS, dementia, retinopathy, a muscle spasm, amigraine, vomiting, dyskinesia, or depression and can be determined bystandard clinical techniques. In addition, in vitro or in vivo assayscan optionally be employed to help identify optimal dosage ranges. Theprecise dose to be employed will also depend on the route ofadministration, and the seriousness of the condition being treated andshould be decided according to the judgment of the practitioner and eachpatient's circumstances in view of, e.g., published clinical studies.Suitable effective dosage amounts, however, range from about 10micrograms to about 2500 milligrams about every 4 h, although they aretypically about 100 mg or less. In one embodiment, the effective dosageamount ranges from about 0.01 milligrams to about 100 milligrams of aBenzoazolylpiperazine Compound about every 4 h, in another embodiment,about 0.020 milligrams to about 50 milligrams about every 4 h, and inanother embodiment, about 0.025 milligrams to about 20 milligrams aboutevery 4 h. The effective dosage amounts described herein refer to totalamounts administered; that is, if more than one BenzoazolylpiperazineCompound is administered, the effective dosage amounts correspond to thetotal amount administered.

Where a cell capable of expressing VR1, mGluR5, or mGluR1 is contactedwith a Benzoazolylpiperazine Compound in vitro, the amount effective forinhibiting the receptor function in a cell will typically range fromabout 0.01 μg/L to about 5 mg/L, in one embodiment, from about 0.01 μg/Lto about 2.5 mg/L, in another embodiment, from about 0.01 μg/L to about0.5 mg/L, and in another embodiment, from about 0.01 μg/L to about 0.25mg/L of a solution or suspension of a pharmaceutically acceptablecarrier or excipient. In one embodiment, the volume of solution orsuspension is from about 1 μL to about 1 mL. In another embodiment, thevolume of solution or suspension is about 200 μL.

Where a cell capable of expressing VR1, mGluR5, or mGluR1 is contactedwith a Benzoazolylpiperazine Compound in vivo, the amount effective forinhibiting the receptor function in a cell will typically range fromabout 0.01 mg to about 100 mg/kg of body weight per day, in oneembodiment, from about 0.1 mg to about 50 mg/kg body weight per day, andin another embodiment, from about 1 mg to about 20 mg/kg of body weightper day.

The Benzoazolylpiperazine Compounds can be assayed in vitro or in vivofor the desired therapeutic or prophylactic activity prior to use inhumans. Animal model systems can be used to demonstrate safety andefficacy.

The present methods for treating or preventing pain, UI, an ulcer, IBD,IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety,epilepsy, stroke, a seizure, a pruritic condition, psychosis, acognitive disorder, a memory deficit, restricted brain function,Huntington's chorea, ALS, dementia, retinopathy, a muscle spasm, amigraine, vomiting, dyskinesia, or depression in an animal in needthereof can further comprise administering to the animal beingadministered a Benzoazolylpiperazine Compound another therapeutic agent.In one embodiment, the other therapeutic agent is administered in aneffective amount.

The present methods for inhibiting VR1 function in a cell capable ofexpressing VR1 can further comprise contacting the cell with aneffective amount of another therapeutic agent.

The present methods for inhibiting mGluR5 function in a cell capable ofexpressing mGluR5 can further comprise contacting the cell with aneffective amount of another therapeutic agent.

The present methods for inhibiting mGluR1 function in a cell capable ofexpressing mGluR1 can further comprise contacting the cell with aneffective amount of another therapeutic agent.

The other therapeutic agent includes, but is not limited to, an opioidagonist, a non-opioid analgesic, a non-steroid anti-inflammatory agent,an antimigraine agent, a Cox-II inhibitor, an antiemetic, a β-adrenergicblocker, an anticonvulsant, an antidepressant, a Ca2+-channel blocker,an anticancer agent, an agent for treating or preventing UI, an agentfor treating or preventing an ulcer, an agent for treating or preventingIBD, an agent for treating or preventing IBS, an agent for treatingaddictive disorder, an agent for treating Parkinson's disease andparkinsonism, an agent for treating anxiety, an agent for treatingepilepsy, an agent for treating a stroke, an agent for treating aseizure, an agent for treating a pruritic condition, an agent fortreating psychosis, an agent for treating Huntington's chorea, an agentfor treating ALS, an agent for treating a cognitive disorder, an agentfor treating a migraine, an agent for treating vomiting, an agent fortreating dyskinesia, or an agent for treating depression, and mixturesthereof.

Effective amounts of the other therapeutic agents are well known tothose skilled in the art. However, it is well within the skilledartisan's purview to determine the other therapeutic agent's optimaleffective-amount range. In one embodiment of the invention, whereanother therapeutic agent is administered to an animal, the effectiveamount of the Benzoazolylpiperazine Compound is less than its effectiveamount would be where the other therapeutic agent is not administered.In this case, without being bound by theory, it is believed that theBenzoazolylpiperazine Compounds and the other therapeutic agent actsynergistically to treat or prevent pain, UI, an ulcer, IBD, IBS, anaddictive disorder, Parkinson's disease, parkinsonism, anxiety,epilepsy, stroke, a seizure, a pruritic condition, psychosis, acognitive disorder, a memory deficit, restricted brain function,Huntington's chorea, ALS, dementia, retinopathy, a muscle spasm, amigraine, vomiting, dyskinesia, or depression.

Examples of useful opioid agonists include, but are not limited to,alfentanil, allylprodine, alphaprodine, anileridine, benzylmorphine,bezitramide, buprenorphine, butorphanol, clonitazene, codeine,desomorphine, dextromoramide, dezocine, diampromide, diamorphone,dihydrocodeine, dihydromorphine, dimenoxadol, dimepheptanol,dimethylthiambutene, dioxaphetyl butyrate, dipipanone, eptazocine,ethoheptazine, ethylmethylthiambutene, ethylmorphine, etonitazenefentanyl, heroin, hydrocodone, hydromorphone, hydroxypethidine,isomethadone, ketobemidone, levorphanol, levophenacylmorphan,lofentanil, meperidine, meptazinol, metazocine, methadone, metopon,morphine, myrophine, nalbuphine, narceine, nicomorphine, norlevorphanol,normethadone, nalorphine, normorphine, norpipanone, opium, oxycodone,oxymorphone, papaveretum, pentazocine, phenadoxone, phenomorphan,phenazocine, phenoperidine, piminodine, piritramide, proheptazine,promedol, properidine, propiram, propoxyphene, sufentanil, tilidine,tramadol, pharmaceutically acceptable salts thereof, and mixturesthereof.

In certain embodiments, the opioid agonist is selected from codeine,hydromorphone, hydrocodone, oxycodone, dihydrocodeine, dihydromorphine,morphine, tramadol, oxymorphone, pharmaceutically acceptable saltsthereof, and mixtures thereof.

Examples of useful non-opioid analgesics include non-steroidalanti-inflammatory agents, such as aspirin, ibuprofen, diclofenac,naproxen, benoxaprofen, flurbiprofen, fenoprofen, flubufen, ketoprofen,indoprofen, piroprofen, carprofen, oxaprozin, pramoprofen, muroprofen,trioxaprofen, suprofen, aminoprofen, tiaprofenic acid, fluprofen,bucloxic acid, indomethacin, sulindac, tolmetin, zomepirac, tiopinac,zidometacin, acemetacin, fentiazac, clidanac, oxpinac, mefenarnic acid,meclofenamic acid, flufenamic acid, niflumic acid, tolfenamic acid,diflurisal, flufenisal, piroxicam, sudoxicam, isoxicam, andpharmaceutically acceptable salts thereof, and mixtures thereof. Othersuitable non-opioid analgesics include the following, non-limiting,chemical classes of analgesic, antipyretic, nonsteroidalanti-inflammatory drugs: salicylic acid derivatives, including aspirin,sodium salicylate, choline magnesium trisalicylate, salsalate,diflunisal, salicylsalicylic acid, sulfasalazine, and olsalazin;para-aminophennol derivatives including acetaminophen and phenacetin;indole and indene acetic acids, including indomethacin, sulindac, andetodolac; heteroaryl acetic acids, including tolmetin, diclofenac, andketorolac; anthranilic acids (fenamates), including mefenamic acid andmeclofenamic acid;. enolic acids, including oxicams (piroxicam,tenoxicam), and pyrazolidinediones (phenylbutazone, oxyphenthartazone);and alkanones, including nabumetone. For a more detailed description ofthe NSAIDs, see Paul A. Insel, Analgesic-Antipyretic andAnti-inflammatory Agents and Drugs Employed in the Treatment of Gout, inGoodman & Gilman's The Pharmacological Basis of Therapeutics 617-57(Perry B. Molinhoff and Raymond W. Ruddon eds., 9^(th) ed. 1996) andGlen R. Hanson, Analgesic, Antipyretic and Anti-Inflammatory Drugs inRemington: The Science and Practice ofPharmacy Vol II 1196-1221 (A.R.Gennaro ed. 19th ed. 1995) which are hereby incorporated by reference intheir entireties.

Examples of useful Cox-II inhibitors and 5-lipoxygenase inhibitors, aswell as combinations thereof, are described in U.S. Pat. No. 6,136,839,which is hereby incorporated by reference in its entirety. Examples ofuseful Cox-II inhibitors include, but are not limited to, rofecoxib andcelecoxib.

Examples of useful antimigraine agents include, but are not limited to,alpiropride, dihydroergotamine, dolasetron, ergocornine, ergocorninine,ergocryptine, ergot, ergotamine, flumedroxone acetate, fonazine,lisuride, lomerizine, methysergide oxetorone, pizotyline, and mixturesthereof.

The other therapeutic agent can also be an agent useful for reducing anypotential side effects of a Benzoazolylpiperazine Compounds. Forexample, the other therapeutic agent can be an antiemetic agent.Examples of useful antiemetic agents include, but are not limited to,metoclopromide, domperidone, prochlorperazine, promethazine,chlorpromazine, trimethobenzamide, ondansetron, granisetron,hydroxyzine, acetylleucine monoethanolamine, alizapride, azasetron,benzquinamide, bietanautine, bromopride, buclizine, clebopride,cyclizine, dimenhydrinate, diphenidol, dolasetron, meclizine,methallatal, metopimazine, nabilone, oxyperndyl, pipamazine,scopolamine, sulpiride, tetrahydrocannabinol, thiethylperazine,thioproperazine, tropisetron, and mixtures thereof.

Examples of useful β-adrenergic blockers include, but are not limitedto, acebutolol, alprenolol, amosulabol, arotinolol, atenolol, befinolol,betaxolol, bevantolol, bisoprolol, bopindolol, bucumolol, bufetolol,bufuralol, bunitrolol, bupranolol, butidrine hydrochloride, butofilolol,carazolol, carteolol, carvedilol, celiprolol, cetamolol, cloranolol,dilevalol, epanolol, esmolol, indenolol, labetalol, levobunolol,mepindolol, metipranolol, metoprolol, moprolol, nadolol, nadoxolol,nebivalol, nifenalol, nipradilol, oxprenolol, penbutolol, pindolol,practolol, pronethalol, propranolol, sotalol, sulfinalol, talinolol,tertatolol, tilisolol, timolol, toliprolol, and xibenolol.

Examples of useful anticonvulsants include, but are not limited to,acetylpheneturide, albutoin, aloxidone, aminoglutethimide,4-amino-3-hydroxybutyric acid, atrolactamide, beclamide, buramate,calcium bromide, carbamazepine, cinromide, clomethiazole, clonazepam,decimemide, diethadione, dimethadione, doxenitroin, eterobarb,ethadione, ethosuximide, ethotoin, felbamate, fluoresone, gabapentin,5-hydroxytryptophan, lamotrigine, magnesium bromide, magnesium sulfate,mephenytoin, mephobarbital, metharbital, methetoin, methsuximide,5-methyl-5-(3-phenanthryl)-hydantoin, 3-methyl-5-phenylhydantoin,narcobarbital, nimetazepam, nitrazepam, oxcarbazepine, paramethadione,phenacemide, phenetharbital, pheneturide, phenobarbital, phensuximide,phenylmethylbarbituric acid, phenytoin, phethenylate sodium, potassiumbromide, pregabaline, primidone, progabide, sodium bromide, solanum,strontium bromide, suclofenide, sulthiame, tetrantoin, tiagabine,topiramate, trimethadione, valproic acid, valpromide, vigabatrin, andzonisamide.

Examples of useful antidepressants include, but are not limited to,binedaline, caroxazone, citalopram, dimethazan, fencamine, indalpine,indeloxazine hydrocholoride, nefopam, nomifensine, oxitriptan,oxypertine, paroxetine, sertraline, thiazesim, trazodone, benmoxine,iproclozide, iproniazid, isocarboxazid, nialamide, octamoxin,phenelzine, cotinine, rolicyprine, rolipram, maprotiline, metralindole,mianserin, mirtazepine, adinazolam, amitriptyline, amitriptylinoxide,amoxapine, butriptyline, clomipramine, demexiptiline, desipramine,dibenzepin, dimetacrine, dothiepin, doxepin, fluacizine, imipramine,imipramine N-oxide, iprindole, lofepramine, melitracen, metapramine,nortriptyline, noxiptilin, opipramol, pizotyline, propizepine,protriptyline, quinupramine, tianeptine, trimipramine, adrafinil,benactyzine, bupropion, butacetin, dioxadrol, duloxetine, etoperidone,febarbamate, femoxetine, fenpentadiol, fluoxetine, fluvoxamine,hematoporphyrin, hypericin, levophacetoperane, medifoxamine,milnacipran, minaprine, moclobemide, nefazodone, oxaflozane, piberaline,prolintane, pyrisuccideanol, ritanserin, roxindole, rubidium chloride,sulpiride, tandospirone, thozalinone, tofenacin, toloxatone,tranylcypromine, L-tryptophan, venlafaxine, viloxazine, and zimeldine.

Examples of useful Ca2+-channel blockers include, but are not limitedto, bepridil, clentiazem, diltiazem, fendiline, gallopamil, mibefradil,prenylamine, semotiadil, terodiline, verapamil, amlodipine, aranidipine,barnidipine, benidipine, cilnidipine, efonidipine, elgodipine,felodipine, isradipine, lacidipine, lercanidipine, manidipine,nicardipine, nifedipine, nilvadipine, nimodipine, nisoldipine,nitrendipine, cinnarizine, flunarizine, lidoflazine, lomerizine,bencyclane, etafenone, fantofarone, and perhexiline.

Examples of useful anticancer agents include, but are not limited to,acivicin, aclarubicin, acodazole hydrochloride, acronine, adozelesin,aldesleukin, altretamine, ambomycin, ametantrone acetate,aminoglutethimide, amsacrine, anastrozole, anthramycin, asparaginase,asperlin, azacitidine, azetepa, azotomycin, batimastat, benzodepa,bicalutamide, bisantrene hydrochloride, bisnafide dimesylate, bizelesin,bleomycin sulfate, brequinar sodium, bropirimine, busulfan,cactinomycin, calusterone, caracemide, carbetimer, carboplatin,carmustine, carubicin hydrochloride, carzelesin, cedefingol,chlorambucil, cirolemycin, cisplatin, cladribine, crisnatol mesylate,cyclophosphamide, cytarabine, dacarbazine, dactinomycin, daunorubicinhydrochloride, decitabine, dexormaplatin, dezaguanine, dezaguaninemesylate, diaziquone, docetaxel, doxorubicin, doxorubicin hydrochloride,droloxifene, droloxifene citrate, dromostanolone propionate, duazomycin,edatrexate, eflornithine hydrochloride, elsamitrucin, enloplatin,enpromate, epipropidine, epirubicin hydrochloride, erbulozole,esorubicin hydrochloride, estramustine, estramustine phosphate sodium,etanidazole, etoposide, etoposide phosphate, etoprine, fadrozolehydrochloride, fazarabine, fenretinide, floxuridine, fludarabinephosphate, fluorouracil, flurocitabine, fosquidone, fostriecin sodium,gemcitabine, gemcitabine hydrochloride, hydroxyurea, idarubicinhydrochloride, ifosfamide, ilmofosine, interleukin II (includingrecombinant interleukin II or rIL2), interferon alfa-2a, interferonalfa-2b, interferon alfa-n1, interferon alfa-n3, interferon beta-I a,interferon gamma-I b, iproplatin, irinotecan hydrochloride, lanreotideacetate, letrozole, leuprolide acetate, liarozole hydrochloride,lometrexol sodium, lomustine, losoxantrone hydrochloride, masoprocol,maytansine, mechlorethamine hydrochloride, megestrol acetate,melengestrol acetate, melphalan, menogaril, mercaptopurine,methotrexate, methotrexate sodium, metoprine, meturedepa, mitindomide,mitocarcin, mitocromin, mitogillin, mitomalcin, mitomycin, mitosper,mitotane, mitoxantrone hydrochloride, mycophenolic acid, nocodazole,nogalamycin, ormaplatin, oxisuran, paclitaxel, pegaspargase, peliomycin,pentamustine, peplomycin sulfate, perfosfamide, pipobroman, piposulfan,piroxantrone hydrochloride, plicamycin, plomestane, porfimer sodium,porfiromycin, prednimustine, procarbazine hydrochloride, puromycin,puromycin hydrochloride, pyrazofurin, riboprine, rogletimide, safingol,safingol hydrochloride, semustine, simtrazene, sparfosate sodium,sparsomycin, spirogermanium hydrochloride, spiromustine, spiroplatin,streptonigrin, streptozocin, sulofenur, talisomycin, tecogalan sodium,tegafur, teloxantrone hydrochloride, temoporfin, teniposide, teroxirone,testolactone, thiamiprine, thioguanine, thiotepa, tiazofturin,tirapazamine, toremifene citrate, trestolone acetate, triciribinephosphate, trimetrexate, trimetrexate glucuronate, triptorelin,tubulozole hydrochloride, uracil mustard, uredepa, vapreotide,verteporfin, vinblastine sulfate, vincristine sulfate, vindesine,vindesine sulfate, vinepidine sulfate, vinglycinate sulfate,vinleurosine sulfate, vinorelbine tartrate, vinrosidine sulfate,vinzolidine sulfate, vorozole, zeniplatin, zinostatin, zorubicinhydrochloride.

Examples of other anti-cancer drugs include, but are not limited to,20-epi-1,25 dihydroxyvitamin D3; 5-ethynyluracil; abiraterone;aclarubicin; acylfulvene; adecypenol; adozelesin; aldesleukin; ALL-TKantagonists; altretamine; ambamustine; amidox; amifostine;aminolevulinic acid; amrubicin; amsacrine; anagrelide; anastrozole;andrographolide; angiogenesis inhibitors; antagonist D; antagonist G;antarelix; anti-dorsalizing morphogenetic protein1; antiandrogen,prostatic carcinoma; antiestrogen; antineoplaston; antisenseoligonucleotides; aphidicolin glycinate; apoptosis gene modulators;apoptosis regulators; apurinic acid; ara-CDP-DL-PTBA; argininedeaminase; asulacrine; atamestane; atrimustine; axinastatin 1;axinastatin 2; axinastatin 3; azasetron; azatoxin; azatyrosine; baccatinIII derivatives; balanol; batimastat; BCR/ABL antagonists;benzochlorins; benzoylstaurosporine; beta lactam derivatives;beta-alethine; betaclamycin B; betulinic acid; bFGF inhibitor;bicalutamide; bisantrene; bisaziridinylspermine; bisnafide; bistrateneA; bizelesin; breflate; bropirimine; budotitane; buthionine sulfoximine;calcipotriol; calphostin C; camptothecin derivatives; canarypox IL-2;capecitabine; carboxamide-amino-triazole; carboxyamidotriazole; CaRestM3; CARN 700; cartilage derived inhibitor; carzelesin; casein kinaseinhibitors (ICOS); castanospermine; cecropin B; cetrorelix; chlorlns;chloroquinoxaline sulfonamide; cicaprost; cis-porphyrin; cladribine;clomifene analogues; clotrimazole; collismycin. A; collismycin B;combretastatin A4; combretastatin analogue; conagenin; crambescidin 816;crisnatol; cryptophycin 8; cryptophycin A derivatives; curacin A;cyclopentanthraquinones; cycloplatam; cypemycin; cytarabine ocfosfate;cytolytic factor; cytostatin; dacliximab; decitabine; dehydrodidemnin B;deslorelin; dexamethasone; dexifosfamide; dexrazoxane; dexverapamil;diaziquone; didemnin B; didox; diethylnorspermine;dihydro-5-azacytidine; dihydrotaxol, 9-; dioxamycin; diphenylspiromustine; docetaxel; docosanol; dolasetron; doxifluridine;droloxifene; dronabinol; duocarmycin SA; ebselen; ecomustine;edelfosine; edrecolomab; eflomithine; elemene; emitefur; epirubicin;epristeride; estramustine analogue; estrogen agonists; estrogenantagonists; etanidazole; etoposide phosphate; exemestane; fadrozole;fazarabine; fenretinide; filgrastim; finasteride; flavopiridol;flezelastine; fluasterone; fludarabine; fluorodaunorunicinhydrochloride; forfenimex; formestane; fostriecin; fotemustine;gadolinium texaphyrin; gallium nitrate; galocitabine; ganirelix;gelatinase inhibitors; gemcitabine; glutathione inhibitors; hepsulfam;heregulin; hexamethylene bisacetamide; hypericin; ibandronic acid;idarubicin; idoxifene; idramantone; ilmofosine; ilomastat;imidazoacridones; imiquimod; immunostimulant peptides; insulin-likegrowth factor-1 receptor inhibitor; interferon agonists; interferons;interleukins; iobenguane; iododoxorubicin; ipomeanol, 4-; iroplact;irsogladine; isobengazole; isohomohalicondrin B; itasetron;jasplakinolide; kahalalide F; lamellarin-N triacetate; lanreotide;leinamycin; lenograstim; lentinan sulfate; leptolstatin; letrozole;leukemia inhibiting factor; leukocyte alpha interferon;leuprolide+estrogen+progesterone; leuprorelin; levamisole; liarozole;linear polyamine analogue; lipophilic disaccharide peptide; lipophilicplatinum compounds; lissoclinamide 7; lobaplatin; lombricine;lometrexol; lonidamine; losoxantrone; lovastatin; loxoribine;lurtotecan; lutetium texaphyrin; lysofylline; lytic peptides;maitansine; mannostatin A; marimastat; masoprocol; maspin; matrilysininhibitors; matrix metalloproteinase inhibitors; menogaril; merbarone;meterelin; methioninase; metoclopramide; MIF inhibitor; mifepristone;miltefosine; mirimostim; mismatched double stranded RNA; mitoguazone;mitolactol; mitomycin analogues; mitonafide; mitotoxin fibroblast growthfactor-saporin; mitoxantrone; mofarotene; molgramostim; monoclonalantibody, human chorionic gonadotrophin; monophosphoryl lipidA+myobacterium cell wall sk; mopidamol; multiple drug resistance geneinhibitor; multiple tumor suppressor 1-based therapy; mustard anticanceragent; mycaperoxide B; mycobacterial cell wall extract; myriaporone;N-acetyldinaline; N-substituted benzamides; nafarelin; nagrestip;naloxone+pentazocine; napavin; naphterpin; nartograstim; nedaplatin;nemorubicin; neridronic acid; neutral endopeptidase; nilutamide;nisamycin; nitric oxide modulators; nitroxide antioxidant; nitrullyn;O6-benzylguanine; octreotide; okicenone; oligonucleotides; onapristone;ondansetron; ondansetron; oracin; oral cytokine inducer; ormaplatin;osaterone; oxaliplatin; oxaunomycin; paclitaxel; paclitaxel analogues;paclitaxel derivatives; palauamine; palmitoylrhizoxin; pamidronic acid;panaxytriol; panomifene; parabactin; pazelliptine; pegaspargase;peldesine; pentosan polysulfate sodium; pentostatin; pentrozole;perflubron; perfosfamide; perillyl alcohol; phenazinomycin;phenylacetate; phosphatase inhibitors; picibanil; pilocarpinehydrochloride; pirarubicin; piritrexim; placetin A; placetin B;plasminogen activator inhibitor; platinum complex; platinum compounds;platinum-triamine complex; porfimer sodium; porfiromycin; prednisone;propyl bis-acridone; prostaglandin J2; proteasome inhibitors; proteinA-based immune modulator; protein kinase C inhibitor; protein kinase Cinhibitors, microalgal; protein tyrosine phosphatase inhibitors; purinenucleoside phosphorylase inhibitors; purpurins; pyrazoloacridine;pyridoxylated hemoglobin polyoxyethylene conjugate; raf antagonists;raltitrexed; ramosetron; ras farnesyl protein transferase inhibitors;ras inhibitors; ras-GAP inhibitor; retelliptine demethylated; rhenium Re186 etidronate; rhizoxin; ribozymes; RII retinamide; rogletimide;rohitukine; romurtide; roquinimex; rubiginone B 1; ruboxyl; safingol;saintopin; SarCNU; sarcophytol A; sargramostim; Sdi 1 mimetics;semustine; senescence derived inhibitor 1; sense oligonucleotides;signal transduction inhibitors; signal transduction modulators; singlechain antigen binding protein; sizofiran; sobuzoxane; sodiumborocaptate; sodium phenylacetate; solverol; somatomedin bindingprotein; sonermin; sparfosic acid; spicamycin D; spiromustine;splenopentin; spongistatin 1; squalamine; stem cell inhibitor; stem-celldivision inhibitors; stipiamide; stromelysin inhibitors; sulfinosine;superactive vasoactive intestinal peptide antagonist; suradista;suramin; swainsonine; synthetic glycosaminoglycans; tallimustine;tamoxifen methiodide; tauromustine; tazarotene; tecogalan sodium;tegafur; tellurapyrylium; telomerase inhibitors; temoporfin;temozolomide; teniposide; tetrachlorodecaoxide; tetrazomine;thaliblastine; thiocoraline; thrombopoietin; thrombopoietin mimetic;thymalfasin; thymopoietin receptor agonist; thymotrinan; thyroidstimulating hormone; tin ethyl etiopurpurin; tirapazamine; titanocenebichloride; topsentin; toremifene; totipotent stem cell factor;translation inhibitors; tretinoin; triacetyluridine; triciribine;trimetrexate; triptorelin; tropisetron; turosteride; tyrosine kinaseinhibitors; tyrphostins; UBC inhibitors; ubenimex; urogenitalsinus-derived growth inhibitory factor; urokinase receptor antagonists;vapreotide; variolin B; vector system, erythrocyte gene therapy;velaresol; veramine; verdins; verteporfin; vinorelbine; vinxaltine;vitaxin; vorozole; zanoterone; zeniplatin; zilascorb; and zinostatinstimalamer.

Examples of useful therapeutic agents for treating or preventing UIinclude, but are not limited to, propantheline, imipramine, hyoscyamine,oxybutynin, and dicyclomine.

Examples of useful therapeutic agents for treating or preventing anulcer include, antacids such as aluminum hydroxide, magnesium hydroxide,sodium bicarbonate, and calcium bicarbonate; sucraflate; bismuthcompounds such as bismuth subsalicylate and bismuth subcitrate; H₂antagonists such as cimetidine, ranitidine, famotidine, and nizatidine;H⁺, K⁺-ATPase inhibitors such as omeprazole, iansoprazole, andlansoprazole; carbenoxolone; misprostol; and antibiotics such astetracycline, metronidazole, timidazole, clarithromycin, andamoxicillin.

Examples of useful therapeutic agents for treating or preventing IBDinclude, but are not limited to, anticholinergic drugs; diphenoxylate;loperamide; deodorized opium tincture; codeine; broad-spectrumantibiotics such as metronidazole; sulfasalazine; olsalazie; mesalamine;prednisone; azathioprine; mercaptopurine; and methotrexate.

Examples of useful therapeutic agents for treating or preventing IBSinclude, but are not limited to, propantheline; muscarine receptorantogonists such as pirenzapine, methoctramine, ipratropium, tiotropium,scopolamine, methscopolamine, homatropine, homatropine methylbromide,and methantheline; and antidiarrheal drugs such as diphenoxylate andloperamide.

Examples of useful therapeutic agents for treating or preventing anaddictive disorder include, but are not limited to, methadone,desipramine, amantadine, fluoxetine, buprenorphine, an opiate agonist,3-phenoxypyridine, levomethadyl acetate hydrochloride, and serotoninantagonists.

Examples of useful therapeutic agents for treating or preventingParkinson's disease and parkinsonism include, but are not limited to,carbidopa/levodopa, pergolide, bromocriptine, ropinirole, pramipexole,entacapone, tolcapone, selegiline, amantadine, and trihexyphenidylhydrochloride.

Examples of useful therapeutic agents for treating or preventing anxietyinclude, but are not limited to, benzodiazepines, such as alprazolam,brotizolam, chlordiazepoxide, clobazam, clonazepam, clorazepate,demoxepam, diazepam, estazolam, flumazenil, flurazepam, halazepam,lorazepam, midazolam, nitrazepam, nordazepam, oxazepam, prazepam,quazepam, temazepam, and triazolam; non-benzodiazepine agents, such asbuspirone, gepirone, ipsaprione, tiospirone, zolpicone, zolpidem, andzaleplon; tranquilizers, such as barbituates, e.g., amobarbital,aprobarbital, butabarbital, butalbital, mephobarbital, methohexital,pentobarbital, phenobarbital, secobarbital, and thiopental; andpropanediol carbamates, such as meprobamate and tybamate.

Examples of useful therapeutic agents for treating or preventingepilepsy include, but are not limited to, carbamazepine, ethosuximide,gabapentin, lamotrignine, phenobarbital, phenytoin, primidone, valproicacid, trimethadione, bemzodiaepines, gabapentin, lamotrigine, γ-vinylGABA, acetazolamide, and felbamate.

Examples of useful therapeutic agents for treating or preventing strokeinclude, but are not limited to, anticoagulants such as heparin, agentsthat break up clots such as streptokinase or tissue plasminogenactivator, agents that reduce swelling such as mannitol orcorticosteroids, and acetylsalicylic acid.

Examples of useful therapeutic agents for treating or preventing aseizure include, but are not limited to, carbamazepine, ethosuximide,gabapentin, lamotrignine, phenobarbital, phenytoin, primidone, valproicacid, trimethadione, bemzodiaepines, gabapentin, lamotrigine, γ-vinylGABA, acetazolamide, and felbamate.

Examples of useful therapeutic agents for treating or preventing apruritic condition include, but are not limited to, naltrexone;nalmefene; danazol; tricyclics such as amitriptyline, imipramine, anddoxepin; antidepressants such as those given below, menthol; camphor;phenol; pramoxine; capsaicin; tar; steroids; and antihistamines.

Examples of useful therapeutic agents for treating or preventingpsychosis include, but are not limited to, phenothiazines such aschlorpromazine hydrochloride, mesoridazine besylate, and thoridazinehydrochloride; thioxanthenes such as chloroprothixene and thiothixenehydrochloride; clozapine; risperidone; olanzapine; quetiapine;quetiapine fumarate; haloperidol; haloperidol decanoate; loxapinesuccinate; molindone hydrochloride; pimozide; and ziprasidone.

Examples of useful therapeutic agents for treating or preventingHuntington's chorea include, but are not limited to, haloperidol andpimozide.

Examples of useful therapeutic agents for treating or preventing ALSinclude, but are not limited to, baclofen, neurotrophic factors,riluzole, tizanidine, benzodiazepines such as clonazepan and dantrolene.

Examples of useful therapeutic agents for treating or preventingcognitive disorders include, but are not limited to, agents for treatingor preventing dementia such as tacrine; donepezil; ibuprofen;antipsychotic drugs such as thioridazine and haloperidol; andantidepressant drugs such as those given below.

Examples of usefil therapeutic agents for treating or preventing amigraine include, but are not limited to, sumatriptan; methysergide;ergotamine; caffeine; and beta-blockers such as propranolol, verapamil,and divalproex.

Examples of useful therapeutic agents for treating or preventingvomiting include, but are not limited to, 5-HT₃ receptor antagonistssuch as ondansetron, dolasetron, granisetron, and tropisetron; dopaminereceptor antagonists such as prochlorperazine, thiethylperazine,chlorpromazin, metoclopramide, and domperidone; glucocorticoids such asdexamethasone; and benzodiazepines such as lorazepam and alprazolam.

Examples of useful therapeutic agents for treating or preventingdyskinesia include, but are not limited to, reserpine and tetrabenazine.

Examples of usefil therapeutic agents for treating or preventingdepression include, but are not limited to, tricyclic antidepressantssuch as amitryptyline, amoxapine, bupropion, clomipramine, desipramine,doxepin, imipramine, maprotilinr, nefazadone, nortriptyline,protriptyline, trazodone, trimipramine, and venlaflaxine; selectiveserotonin reuptake inhibitors such as fluoxetine, fluvoxamine,paroxetine, and setraline; monoamine oxidase inhibitors such asisocarboxazid, pargyline, phenelzine, and tranylcypromine; andpsychostimulants such as dextroamphetamine and methylphenidate.

A Benzoazolylpiperazine Compound and the other therapeutic agent can actadditively or, in one embodiment, synergistically. In one embodiment, aBenzoazolylpiperazine Compound is administered concurrently with anothertherapeutic agent. In one embodiment, a composition comprising aneffective amount of a Benzoazolylpiperazine Compound and an effectiveamount of another therapeutic agent can be administered. Alternatively,a composition comprising an effective amount of a BenzoazolylpiperazineCompound and a different composition comprising an effective amount ofanother therapeutic agent can be concurrently administered. In anotherembodiment, an effective amount of a Benzoazolylpiperazine Compound isadministered prior or subsequent to administration of an effectiveamount of another therapeutic agent. In this embodiment, theBenzoazolylpiperazine Compound is administered while the othertherapeutic agent exerts its therapeutic effect, or the othertherapeutic agent is administered while the BenzoazolylpiperazineCompound exerts its preventative or therapeutic effect for treating orpreventing a Condition in an animal.

A composition of the invention is prepared by a method comprisingadmixing a Benzoazolylpiperazine Compound and a pharmaceuticallyacceptable carrier or excipient. Admixing can be accomplished usingmethods well known for admixing a compound (or salt) and apharmaceutically acceptable vehicle. In one embodiment, theBenzoazolylpiperazine Compound is present in the composition in aneffective amount.

4.3.2 Kits

The invention encompasses kits that can simplify the administration of aBenzoazolylpiperazine Compound to an animal.

A typical kit of the invention comprises a unit dosage form of aBenzoazolylpiperazine Compound. In one embodiment, the unit dosage formis a container, which can be sterile, containing an effective amount ofa Benzoazolylpiperazine Compound and a pharmaceutically acceptablevehicle. The kit can further comprise a label or printed instructionsinstructing the use of the Benzoazolylpiperazine Compound to treat pain,UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease,parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruriticcondition, psychosis, a cognitive disorder, a memory deficit, restrictedbrain function, Huntington's chorea, ALS, dementia, retinopathy, amuscle spasm, a migraine, vomiting, dyskinesia, or depression. The kitcan also further comprise a unit dosage form of another therapeuticagent, for example, a container containing an effective amount of theother therapeutic agent. In one embodiment, the kit comprises acontainer containing an effective amount of a BenzoazolylpiperazineCompound and an effective amount of another therapeutic agent. Examplesof other therapeutic agents include, but are not limited to, thoselisted above.

Kits of the invention can further comprise a device that is useful foradministering the unit dosage forms. Examples of such a device includes,but are not limited to, a syringe, a drip bag, a patch, an inhaler, andan enema bag.

The following examples are set forth to assist in understanding theinvention and should not, of course, be construed as specificallylimiting the invention described and claimed herein. Such variations ofthe invention, including the substitution of all equivalents now knownor later developed, which would be within the purview of those skilledin the art, and changes in formulation or minor changes in experimentaldesign, are to be considered to fall within the scope of the inventionincorporated herein.

5. EXAMPLES 5.1. Example 1 Synthesis of Benzoazolylpiperazine Compoundsof Formula (Ia) AAM, AAS, AAQ, AAP, AYF, AYD, AZW, AZZ, AYH, AYE, AYI,AYK, AYG, AYC, AZA, AZD, AYN, and AYM

A solution of of 2-chloro-3-X-pyridine 1 (about 0.5 M -about 1 M) and 1eq. of 2-Q-piperazine 2 in DMSO was heated to about 140° C. withstirring for about 2 to 4 h. The resulting reaction mixture was thencooled to room temperature and the DMSO was removed under reducedpressure to provide compound 3.

In a separate flask a solution of 0.75 eq. of chloroformate 4 indichloromethane (DCM) (0.04M) was cooled to 0° C. and 0.75 eq. of5-Z-6-Y-benzothiazol-2-ylamine 5 was slowly added to the cooled solutionof chloroformate 4. The resulting reaction mixture was stirred at 0° C.for 5 min. and then 5 eq. of triethylamine was added to the reactionmixture. The reaction mixture was then warmed to room temperature andconcentrated under reduced pressure at 40° C. to provide compound 6.

Compound 6 was dissolved in DCM (0.1 M) and 1 eq. of 3 as a 1 M solutionin DCM was added to the solution of compound 6 at room temperature andthe resulting reaction mixture was allowed to stir for about 10 min. Thereaction mixture was then concentrated under reduced pressure at 40° C.to provide the Benzoazolylpiperazine Compound of formula (Ia). TheBenzoazolylpiperazine Compound of formula (Ia) was purified using asilica gel column eluted with 5:95 ethyl acetate/hexane.

Table XXIII lists the Benzoazolylpiperazine Compounds that were preparedaccording to the method of Example 1.

TABLE XXIII Benzoazolylpiperazine Compound X Q Y Z AAM —Cl —H —Cl —H AAS—Cl —H —OCH₂CH₃ —H AAQ —Cl —H —CF₃ —H AAP —Cl —H —CH₃ —H AYF —Cl (R)—CH₃—Br —H AYD —Cl (R)—CH₃ —H —H AZW —CF₃ (R)—CH₃ —Cl —H AZZ —CF₃ (R)—CH₃—CH₃ —H AYH —Cl (R)—CH₃ —CH₃ —H AYE —Cl (R)—CH₃ —Cl —H AYI —Cl (R)—CH₃—CF₃ —H AYK —Cl (R)—CH₃ —OCH₂CH₃ —H AYG —Cl (R)—CH₃ —F —H AYC —Cl(R)—CH₃ —CH₃ —CH₃ AZA —CH₃ (R)—CH₃ —Cl —H AZD —CH₃ (R)—CH₃ —CH₃ —H AYN—Cl (R)—CH₃ —CH(CH₃)₂ —H AYM —Cl (R)—CH₃ —C(CH₃)₃ —H (R)—CH₃ means thatthe carbon atom to which the methyl group is attached is in the (R)configuration.

The identity of Compound AAM was confirmed using H¹ NMR.

Compound AAM: ¹H NMR (400 MHz, CDCl₃), δ8.24-8.19 (m, 1H), 7.77-7.76 (m,1H), 7.67-7.64 (m, 1H), 7.57-7.54 (m, 1H), 7.38-7.36 (m, 1H), 6.95-6.90(m, 1H), 3.77-3.75 (m, 4H), 3.45-3.42 (m, 4H).

The identity of Compound AAS was confirmed using H¹ NMR.

Compound AAS: ¹H NMR (400 MHz, CDCl₃), δ10.17 (s, 1H), 8.19-8.15 (m,1H), 7.61-7.58 (m, 1H), 7.51-7.46 (m,. 1H), 7.28-7.22 (m, 1H), 6.98-6.95(m, 6.89-6.86 (m, 1H), 4.11-4.04 (m, 2H), 3.77-3.71 (m, 4H), 3.37-3.34(m, 4H), 1.43 (t, 3H).

The identity of Compound AAQ was confirmed using H¹ NMR.

Compound AAQ: ¹H NMR (400 MHz, CDCl₃): δ8.22-8.19 (m, 1H), 8.09-8.05 (m,1H), 7.76-7.71 (m, 1H), 7.66-7.64 (m, 2H), 6.94-6.91 (m, 1H), 3.80-3.75(m, 4H), 3.47-3.45 (m, 4H).

The identity of Compound AAP was confirmed using H¹ NMR.

Compound AAP: ¹H NMR (CDCl₃), δ8.22-8.20 (m, 1H), 7.65-7.63 (m, 1H),7.57-7.55 (m, 1H), 7.52-7.48 (m, 1H), 7.22-7.18 (m, 1H), 6.92-6.87 (m,1H), 3.78-3.76 (m, 4H), 3.45-3.42 (m, 4H), 2.46 (s, 3H).

The identity of Compound AYF was confirmed using H¹ NMR.

Compound AYF: ¹H NMR (CDCl₃), δ 8.23-8.20 (m, 1H), 7.93-7.90 (m, 1H),7.67-7.62 (m, 1H), 7.54-7.50 (m, 2H), 6.95-6.91 (m, 1H), 4.45 (bs, 1H),4.11-4.05 (m, 1H), 3.86-3.76 (m, 2H), 3.57-3.46 (m, 1H), 3.12-3.06 (m,1H), 3.02-2.94 (m, 1), 1.50 (d, 3H, J=6.8).

The identity of Compound AYD was confirmed using H¹ NMR and massspectrometry.

Compound AYD: ¹H NMR (CDCl₃), δ 8.83 (br, 1H), 8.24-8.20 (m, 1H),7.81-7.74 (m, 1H), 7.68-759 (m, 2H), 7.48-7.38 (m, 1H), 7.33-7.24 (m, 2H+CHCl₃), 696-6.87 (m, 1H), 4.55-4.43 (m, 1H), 4.17-4.06 (m, 1H),3.89-3.75 (m, 2H), 3.58-3.42 (m, 1H), 3.16-2.89 (m, 1H), 1.45 (d, 3H,J=6.8 Hz).

(M+1) m/z: 388.0.

The identity of Compound AZW was confirmed using H¹ NMR.

Compound AZW: ¹H NMR (CDCl₃), δ8.49-8.45 (m, 1H), 7.94-7.90 (m, 1H),7.57-7.54 (m, 1H), 7.52-7.46 (m, 1H), 7.22-7.18 (m, 1H), 7.11-7.06 (m,1H), 4.46 (bs, 1H), 4.09-4.00 (m, 1H), 3.52-3.42 (m, 2H), 3.38-3.33 (m,1H), 3.25-3.19 (m, 1H), 3.04-2.96 (m, 1H), 1.39 (d, 3H, J=6.8).

The identity of Compound AZZ was confirmed using H¹ NMR.

Compound AZZ: ¹H NMR (CDCl₃), δ8.50-8.46 (m, 1H), 7.94-7.91 (m, 1H),7.55 (bs, 1H), 7.51-7.47 (m, 1H), 7.21-7.17 (m, 1H), 7.11-7.06 (m, 1H),4.45 (bs, 1H), 4.09-4.01 (m, 1H), 3.53-3.45 (m, 2H), 3.41-3.34 (m, 1H),3.26-3.20 (m, 1H), 3.07-2.95 (m, 1H), 2.46 (s, 3H), 1.38 (d, 3H, J=6.7).

The identity of Compound AYH was confirmed using H¹ NMR.

Compound AYH: ¹H NMR (CDC₃), δ8.71 (bs, 1H), 8.24-8.20 (m, 1H), 7.67-762(m, 1H), 7.58 (bs, 1H), 7.55-7.49 (m, 1H), 7.25-7.19 (m, 1H), 6.94-6.89(m, 1H), 4.46 (bs, 1H), 4.14-4.06 (m, 1H), 3.86-3.74 (M, 2H), 3.56-3.43(m, 1H), 3.13-3.05 (m, 1H), 3.03-2.95 (m, 1H), 2.47 (s, 3H), 1.64 (s,3H), 1.47 (d, 3H, J=7.0).

The identity of Compound AYE was confirmed using H¹ NMR.

Compound AYE: ¹H NMR (CDCl₃), δ8.37 (bs, 1H), 8.24-8.21 (m, 1H),7.77-7.75 (m, 1H), 7.67-7.64 (m, 1H), 7.61-7.57 (m, 1H), 7.39-7.35 (m,1H), 6.95-6.90 (m, 1H), 4.40 (bs, 1H), 4.15-4.01 (m, 1H), 3.90-3.77 (m,1H), 3.58-3.47 (m, 1H), 3.14-3.07 (m, 1H), 3.05-2.96 (m, 1H), 1.51 (d,3H, J=6.8).

The identity of Compound AYI was confirmed using H¹ NMR.

Compound AYI: ¹H NMR (CDCl₃), δ9.31 (bs, 1H), 8.22-8.19 (m, 1H), 8.08(bs, 1H), 7.76-7.70 (m, 1H), 7.68-7.61 (m, 2H), 6.94-6.89 (m, 1H), 4.46(bs, 1H), 4.11-4.02 (m, 1H), 3.85-3.74 (m, 2H), 3.59-3.48 (m, 1H),3.12-3.05 (m, 1H), 3.02-2.92 (m, 1H), 1.49 (d, 3H, J=6.8).

The identity of Compound AYK was confirmed using H¹ NMR.

Compound AYK: ¹H NMR (CDCl₃), δ9.40 (bs, 1H), 8.22-8.18 (m, 1H),7.64-7.60 (m, 1H), 7.57-7.51 (m, 1H), 7.30-7.25 (m, 1H+CHC1₃), 7.03-6.97(m, 1H), 6.93-6.88 (m, 1H), 4.45 (bs, 1H), 4.14-4.00 (m, 3H), 3.81-3.69(m, 2H), 3.53-3.43 (m, 1H), 3.09-3.02 (m, 1H), 3.00-2.91 (m, 1H),1.48-1.43 (m, 6H).

The identity of Compound AYG was confirmed using H¹ NMR.

Compound AYG: ¹H NMR (CDCl₃), δ8.41 (bs, 1H), 8.24-8.20 (m, 1H),7.68-7.56 (m, 2H), 7.52-7.46 (m, 1H), 7.18-7.11 (m, 1H), 6.95-6.90 (m,1H). 4.41 (bs, 1H), 4.09-4.02 (m, 1H), 3.89-3.77 (m, 2H), 3.58-3.49 (m,1H), 3.14-307 (m, 1H), 3.05-2.96 (m, 1H), 1.5 (d, 3H, J=6.8).

The identity of Compound AYC was confirmed using H¹ NMR.

Compound AYC: ¹H NMR (CDCl₃), δ8.23-8.19 (m, 1H), 765-7.61 (m, 1H), 7.52(bs, 1H), 7.40 (bs, 1H), 6.93-6.88 (m, 1H), 4.50 (bs, 1H), 4.17-4.06 (m,1H), 3.84-3.73 (m, 2H), 3.56-3.44 (m, 1H), 3.11-3.03 (m, 1H), 3.01-2.92(m, 1H), 2.36 (s, 6H), 1.48 (d., 3H, J=6.8).

The identity of Compound AZA was confirmed using H¹ NMR.

Compound AZA: ¹H NMR (CDCl₃), δ8.93 (bs, 1H), 8.17-8.14 (m, 1H),8.00-7.96 (m, 1H), 7.77 (bs, 1H), 7.60-7.53 (m, 1H), 7.41-7.33 (m, 1H),4.49 (bs, 1H), 4.16-4.06 (m, 1H), 4.00-3.94 (m, 2H), 3.57-3.46 (m, 1H),3.19-3.11 (m, 1H), 3.07-2.98 (m, 1H), 1.70 (s, 3H), 1.47 (d, 3H, J=6.8).

The identity of Compound AZD was confirmed using H¹ NMR.

Compound AZD: ¹H NMR (CDCl₃), δ8.68 (bs, 1H), 8.21-8.18 (m, 1H),7.61-7.43 (m, 3H), 7.24-7.19 (m, 1H), 6.94-6.90 (m, 1H), 4.45 (bs, 1H),4.13-4.04 (m, 1H), 3.54-3.41 (m, 2H), 3.37-3.32 (m, 1H), 3.12-3.04 (m,1H), 3.64-2.90 (m 1H), 2.46 (s, 3H), 2.35 (s, 3H), 1.48 (d, 3H, J=6.8).

The identity of Compound AYN was confirmed using H¹ NMR.

Compound AYN: ¹H NMR (CDCl₃), δ8.20-8.18 (m, 1 H), 7.64-7.59 (m, 1 H),7.58-7.50 (m, 1H), 7.29-7.25 (m, 1H+CHCl₃), 6.91-6.87 (m, 1H), 4.49 (bs,1H), 4.14-4.05 (m, 1H), 3.79-3.68 (m, 2H), 3.07-2.89 (m, 3H), 1.44 (d,3H, J=6.8), 1.31 (d, 3H, =7.0).

The identity of Compound AYM was confirmed using H¹ NMR.

Compound AYM: ¹H NMR (CDCl₃), δ8.24-8.20 (m, 1H), 7.76 (bs, 1H),7.66-7.62 (m, 1H), 7.55-7.52 (m,. 1H), 7.49-7.43 (m, 1H), 6.94-6.89 (m,1H), 4.46 (bs, 1H), 4.16-4.07 (m, 1H), 3.87-3.73 (m, 2H), 3.56-3.45 (m,1H), 3.14-3.05 (m, 1H), 3.04-2.91 (m, 1H), 1.49 (d, 3H, J=6.8), 1.40 (s,9H).:

5.2. Example 2 Synthesis of Benzoazolylpiperazine Compounds of Formula(Ib) BDJ and BDG

Compounds BDJ and BDG were prepared by a method analogous to that usedin Example 1 except that 2, 3-dichloropyrazine was used in place of2-chloro-3-X-pyridine 1. In the preparation of Compound BDJ, the2-Q-piperazine 2 was (R)-2-methylpiperidine and the5-Z-6-Y-benzothiazol-2-ylamine 5 was 6-methyl benzothiazol-2-ylamine. Inthe preparation of Compound BDG, the 2-Q-piperazine 2 was(R)-2-methylpiperidine and the 5-Z-6-Y-benzothiazol-2-ylamine 5 was6-chloro benzothiazol-2-ylamine.

The identity of Compound BDJ was confirmed using H¹ NMR.

Compound BDJ: ¹H NMR (CDCl₃), δ8.16-8.13 (m, 1 H), 7.96-7.93 (m, 1H),7.56 (bs, 1H), 7.47 (bs, 1H), 7.22-7.18 (m, 1H), 4.56 (bs, 1H),4.19-4.13 (m, 1H), 3.94-3.85 (m, 2H), 3.49-3.41 (m, 1H), 3.13-3.06 (m,1H), 3.01-2.94 (m, 1H), 2.45 (s, 3H), 1.41 (d, 3H, J=6.9).

The identity of Compound BDG was confirmed using H¹ NMR.

Compound BDG: ¹H NMR (CDCl₃), δ8.66 (bs, 1H), 8.17-8.15 (m, 1H),8.00-7.97 (m, 1H), 7.76 (bs, 1H), 7.59-7.54 (m, 1H), 7.40-7.35 (m, 1H),4.47 (bs, 1H), 4.16-4.07 (m, 1H), 4.02-3.92 (m, 2H), 3.57-3.48 (m, 1H),3.20-3.13 (m, 1H), 3.09-2.98 (m, 1H), 1.48 (d, 3H, J=6.8).

5.3. Example 3 Synthesis of Benzoazolylpiperazine Compounds of Formula(Ib) BIL, BII, and BJE

Compounds BIL BII, and BJE were prepared by a method analogous to thatused in Example 1 except that 4,5-dichlorothiadiazole was used in placeof 2-chloro-3-X-pyridine 1 to make Compounds BIL and BII and4-methyl-5-chlorothiadiazole was used to make Compound BJE. In thepreparation of Compound BIL, the 2-Q-piperazine 2 was(R)-2-methylpiperidine and the 5-Z-6-Y-benzothiazol-2-ylamine 5 was6-methyl benzothiazol-2-ylamine. In the preparation of Compounds BII,and BJE the 2-Q-piperazine 2 was (R)-2-methylpiperidine and the5-Z-6-Y-benzothiazol-2-ylamine 5 was 6-chloro benzothiazol-2-ylamine.

The identity of Compound BIL was confirmed using H¹ NMR.

Compound BIL: ¹H NMR (CDCl₃), δ7.54 (bs, 1H), 7.49-7.42 (m, 1H),7.24-7.17 (m, 1H), 4.55 (bs, 1H), 4.24-4.15 (m, 1H), 4.02-3.89 (m, 2H),3.54-3.39 (m, 1H), 3.21-3.12 (m, 1H), 3.11-3.02 (m, 1H), 2.46 (s, 3H),1.46 (d, 3H, J=6.8).

The identity of Compound BII was confirmed using H¹ NMR.

Compound BII: ¹H NMR (CDCl₃), δ8.64 (bs, 1H), 7.75 (bs, 1H), 7.58-7.51(m, 1H), 7.41-7.34 (m, 1H), 4.50 (bs, 1H), 4.18-4.06 (m, 1H), 4.01-3.92(m, 2H), 3.56-3.44 (m, 1H), 3.21-3.13 (m, 1H), 3.12-3.04 (m, 1H), 1.48(d, 3H, J=6.8).

The identity of Compound BJE was confirmed using H¹ NMR.

Compound BJE: ¹H NMR (CDCl₃), δ8.59 (bs, 1H), 7.73 (bs, 1H), 7.53-7.47(m, 1H), 7.41-7.34 (m, 1H), 4.55 (bs, 1H), 4.23-4.14 (m, 1H), 3.59-3.46(m, 1H), 3.43-3.38 (m, 1H). 3.37-3.28 (m, 1H), 3.11-3.02 (m, 1H),3.00-2.90 (m, 1H), 2.65 (s, 3H), 1.61 (d, 3H, J=6.8).

5.4. Example 4 Synthesis of Benzoazolylpiperazine Compound of Formula(IIa) and (IIb) CBG, CAW, CRU, CSE, DIS, DJC, DIQ, CSE, EAA, DZU, CTA,CTW, CRW, and CSB

A solution of 2-chloro-3-X-pyridine 1 (about 0.5 M to about 1M) and 1eq. of 2-Q-piperazine 2 in DMSO was heated to about 140° C. withstirring for about 2 to 4 h. The resulting reaction mixture was thencooled to room temperature and the DMSO was removed under reducedpressure to provide compound 3.

A solution of compound 3 (about 0.25 mmol-about 1 mmol) and 1 eq. ofcompound 7 in about 3 mL of toluene or xylene was heated at atemperature of between about 140° C. and 150° C. for about 3 days. Theresulting reaction mixture was then concentrated under reduced pressureto provide a residue that was purified using flash chromatography(silica gel, gradient elution 2% methanol:DCM to 6% methanol:DCM).

Compound 7, wherein R₁₀ is —H was either commercially available orobtained from commercially available compounds 8 as illustrated below

Compound 8 (about 30 mmol) and carbodiimidazole (CDI) (commerciallyavailable from Sigma-Aldrich, St. Louis, Mo. (www.sigma-aldrich.com))(about 2 eq) was dissolved in THF (about 50 to about 150 mL) and theresulting reaction mixture was heated at reflux temperature for about 4hours. The reaction mixture was then concentrated under reduced pressureto provide a residue. About 50 to about 100 mL of ethyl acetate or ethylacetate/hexane (20:80 to about 40:60) was added to the residue and theresulting insoluble material was collected by filtration and washed withethyl acetate or ethyl acetate/hexane (20:80 to about 40:60) to providecompound 9. Compound 9 was then reacted with POCl₃ according to theprocedure described in J Med. Chem. 40:586-593 (1997) to providecompound 7.

Compound 7, wherein R₁₀ is —CH₃ was obtained from compound 7 wherein R₁₀is —H as illustrated below

NaH (about 2 eq) was added to a solution of a compound of Formula 8wherein R₁₀ is —H in DMF at 0° C. and the resulting mixture was allowedto stir and to warm to room temperature over a period of about one hour.Methyl iodide (about 1.2 eq) was then added to the solution and theresulting reaction mixture was allowed to stir for several minutes.Water was then added to the reaction mixture to produce a precipitate ofcompound 8 wherein R₁₀ is —CH₃ which was filtered, collected, and dried.

Table XXIV lists the Benzoazolylpiperazine Compounds that were preparedaccording to the method of Example 4.

TABLE XXIV Benzoazolylpiperazine Compound R₁₀ Y Z X Q CBG —H -tert-butyl—H —Cl —H CAW —H —CH₃ —CH₃ —Cl —H CRU —H —CH₃ —CH₃ —Cl (R)— CH₃ CRU —H—CH₃ —CH₃ —Cl (S)— CH₃ CSE —H -tert-butyl —H —Cl (R)— CH₃ DIS —CH₃ —CH₃—CH₃ —Cl —H DJC —CH₃ -tert-butyl —H —Cl —H DIQ —CH₃ —H -tert- —Cl —Hbutyl CSE —H -tert-butyl —H —Cl (S)— CH₃ EAA —CH₃ -tert-butyl —H —Cl(R)— CH₃ DZO —CH₃ —H -tert- —Cl (R)— butyl CH₃ CTA —H -tert-butyl —H—CH₃ (R)— CH₃ CTW —H -tert-butyl —H —CF₃ (R)— CH₃ CRW —H —Cl —H —Cl (R)—CH₃ CSB —H —OCH₃ —H —Cl (R)— CH₃ (R)—CH₃ means that the carbon atom towhich the methyl group is attached is in the (R) configuration. (S)—CH₃means that the carbon atom to which the methyl group is attached is inthe (S) configuration.

The identity of Compound CBG was confirmed using H¹ NMR and massspectrometry.

Compound CBG: ¹H NMR (CD₃OD), δ8.21(dd, 1H, J1=1.6 Hz, J2=4.8 Hz);7.77(dd, 1H, J1=1.6 Hz, J2=7.6 Hz); 7.34(d, 1H, J=2 Hz); 7.21(d, 1H,J1=0.4 Hz, J2=8.4 Hz); 7.14(dd, 1H, J1=2 Hz, J2=8.4 Hz); 7.01(dd, 1H,J1=4.8 Hz, J2=7.6 Hz); 3.70(m, 4H); 3.49(m, 4H); 1.37(s, 9H).

MS: 370.2(M+1).

The identity of Compound CAW was confirmed using H¹ NMR and massspectrometry.

Compound CAW: ¹H NMR (CD₃OD), δ 8.25(dd, 1H, J1=1.6 Hz, J2=4.8 Hz);7.82(dd, 1H, J1=1.6 Hz, J2=8 Hz); 7.06(dd, 1H, J1=4.8 Hz, J2=7.6 Hz);3.82(m, 4H); 3.58(m, 4H); 2.38(s, 6H).

MS: 342.1(M+1).

The identity of Compound CRU wherein Q is (R)—CH₃ was confirmed using H¹NMR and mass spectrometry.

Compound CRU wherein Q is (R)—CH₃: ¹H NMR (CD₃OD), δ 8.25(dd, 1H, J1=1.6Hz, J2=4.8 Hz); 7.82(dd, 1H, J1=2 Hz, J2=8 Hz); 7.07(dd, 1H, J1=4.4 Hz,J2=8 Hz); 4.30(m 1H); 3.90(m, 4H); 3.26(dd, 1H, J1=13 Hz, J2=1.6 Hz);3.17(m, 1H); 2.38(s, 6H); 1.59(d, 3H, J=6.8 Hz).

MS: 356.1(M+1).

The identity of Compound CRU wherein Q is (S)—CH₃ was confirmed using H¹NMR and mass spectrometry.

Compound CRU wherein Q is (S)—CH₃: ¹H NMR (CD₃OD), δ 8.25(dd, 1H, J1=1.2Hz, J2=4.4 Hz); 7.81(dd, 1H, J1=1.6 Hz, J2=7.6 Hz); 7.07(dd, 1H, J1=4.8Hz, J2=7.6 Hz); 4.31(m, 1H); 3.88(m, 4H); 3.26(dd, 1H, J1=3.6 Hz, J2=13Hz); 3.16(m, 1H); 2.38(s, 6H); 1.59(d, 3H, J=6.4 Hz).

MS: 356.1(M+1).

The identity of Compound CSE wherein Q is (R)—CH₃ was confirmed using H¹NMR and mass spectrometry.

Compound CSE wherein Q is (R)—CH₃: ¹H NMR (CD₃OD), δ 8.22(dd, 1H, J1=1.6Hz, J2=4.8 Hz0; 7.78(dd, 1H, J1=1.6 Hz, J2=7.6 Hz0; 7.33(dd, 1H, J1=0.8Hz, J2=2 Hz); 7.19(dd, 1H, J1=0.8 Hz, J2=8.4 Hz0; 7.12(dd, 1H, J1=1.6Hz, J2=8.4 Hz); 7.02(dd, 1H, J1=4.8 Hz, J2=8 Hz); 4.37(m, 1H); 3.84(m,3H): 3.58(m, 1H); 3.20(dd, 1H, J1=4 Hz, J2=12 Hz); 3.08(dt, 1H, J1=3.2Hz, J2=12 Hz); 1.45(d, 3H, J=6.4 Hz); 1.37(s, 9H),

MS: 420(M+36).

The identity of Compound DIS was confirmed using H¹ NMR and massspectrometry.

Compound DIS: ¹H NMR (CD₃OD), δ 8.23(dd, 1H, J1=1.6 Hz, J2=4.8 Hz);7.78(dd, 1 h, J1=2 Hz, J2=8 Hz); 727(bs, 1H); 7.14(bs, 1H); 7.02(dd, 1H,J1=4.8 Hz, J2=7.6 Hz); 3.69(s, 3H); 3.56(m, 4H); 3.45(m, 4H); 2.39(s,3H); 2.35(s, 3H).

MS: 356.1(M+1).

The identity of Compound DJC was confirmed using H¹ NMR and massspectrometry.

Compound DJC: ¹H NMR (CD₃OD), δ 8.23(dd, 1H, J1=1.6 Hz, J2=4.8 Hz);7.78(dd, 1H, J1=2 Hz, J2=8 Hz); 7.53(dd, 1H, J1=0.8 Hz, J2=2 Hz); 7.31(dd, 1H, J1=1.6 Hz, J2=8.4 Hz); 7.26(dd, 1H, J1=0.4 Hz, J2=8.4 Hz);7.02(dd, 1H, J1=4.8 Hz, J2=8 Hz); 3.70(s, 3H); 3.57(m, 4H); 3.47(m, 4H);1.39(s, 9H).

MS: 384.1(M+1).

The identity of Compound DIQ was confirmed using H¹ NMR and massspectrometry.

Compound DIQ: ¹H NMR (CD₃OD), δ 8.23(dd, 1H, J1=1.6 Hz, J2=4.8 Hz);7.78(dd, 1H, J1=2 Hz, J2=8 Hz); 7.41(dd, 1H, J1=0.4 Hz, J2=8.4 Hz);7.36(d, 1H, J=1.2 Hz); 7.29(dd, 1H, J1=1.6 Hz, J2=8.4 Hz); 7.02(dd, 1H,J1=4.8 Hz, J2=7.6 Hz); 3.70(s, 3H); 3.57(m, 4H); 3.47(m, 4H); 1.41(s,9H).

MS: 384.1(M+1).

The identity of Compound CSE wherein Q is (S)—CH₃ was confirmed using H¹NMR and mass spectrometry.

Compound CSE wherein Q is (S)—CH₃: ¹H NMR (CD₃OD), δ 8.22(dd, 1H, J1=1.6Hz, J2=4.8 Hz); 7.78(dd, 1H, J1=1.6 Hz, J2=7.6 Hz); 7.34(d, 1H, J=1.6Hz); 7.20(d, 1H, J=8.4 Hz); 7.13(dd, 1H, J1=2 Hz, J2=8.4 Hz); 7.02(dd,1H, J1=4.8 Hz, J2=8 Hz); 4.36(m, 1H); 3.85(m, 3H); 3.60(dt, 1H, J1=2.8Hz, J2=12 Hz); 3.20(dd, 1H, J1=4 Hz, J2=12 Hz); 3.08(dt, 1H, J1=3.2 Hz,J2=13 Hz); 1.45(d, 3H, J=6.4 Hz); 1.37(s, 9H).

MS: 420(M+36).

The identity of Compound EAA wherein Q is (R)—CH₃ was confirmed using H¹NMR and mass spectrometry.

Compound EAA wherein Q is (R)—CH₃: ¹H NMR (DMSO d₆), δ 8.23(dd, 1H,J1=1.6 Hz, J2=2.8 Hz); 7.63(dd, 1H, J1=1.6 Hz, J2=7.6 Hz); 7.61(d, 1H,J1=8.4 Hz); 7.32(dd, 1H, J=2 Hz, J2=8 Hz); 7.26(dd, 1H, J1=1.6 Hz, J2=8Hz); 6.90(dd, 1H, J1=4.8 Hz, J2=8 Hz); 3.80(m, 1H); 3.70(s, 3H);3.69(dd, 1H, J1=2.8 Hz, J2=12 Hz); 3.63(m, 1H) 3.45(m, 2H); 3.35(m, 1H);3.24(dd, 1H, J1=7.6 Hz, J2=12 Hz); 1.43(s, 9H); 1.20(d, 3H, J=6.4 Hz).

MS: 398.1(M+1).

The identity of Compound DZO wherein Q is (R)—CH₃ was confirmed using H¹NMR and mass spectrometry.

Compound DZO wherein Q is (R)—CH₃: ¹H NMR (DMSO d₆), δ 8.23(dd, 1H, J1=2Hz, J2=4.8 Hz); 7.75(d); 7.63(dd, 1H, J1=2 Hz, J2=7.6 Hz); 7.32(dd, 1H,J1=2 Hz, J2=8.4 Hz); 7.20(d, 1H, J=8.4 Hz); 6.89(dd, 1H, J1=4.8 Hz,J2=7.6 Hz); 3.82(m, 1H); 3.68(s, 3H); 3.68(m, 1H); 3.61(m, 1H); 3.48(m,2H); 3.37(m, 1H); 3.28(dd, 1H, J1=8 Hz, J2=12 Hz); 1.41(s, 9H); 1.22(d,3H, J=6.4 Hz).

MS: 398.3(M+1).

The identity of Compound CTA wherein Q is (R)—CH₃ was confirmed using H¹NMR and mass spectrometry.

Compound CTA wherein Q is (R)—CH₃: ¹H NMR (CDCl₃), δ 8.17(d,1H, J=4.8Hz); 7.44(d, 1H, J=7.6 Hz); 7.42(s, 1H); 7.27(d, 1H, J=8.4 Hz); 7.13(d,1H, J=8.4 Hz); 6.91(dd, 1H, J1=4.8 Hz, J2=7.2 Hz); 4.42(m, 1H); 3.97(d,1H, J=12 Hz); 3.62(dt, 1H, J1=3.2 Hz, J2=12 Hz); 3.47(d, 1H, J=12 Hz);3.33(d, 1H, J=13 Hz); 3.18(dd, 1H, J1=3.2 Hz, J2=12 Hz); 3.06(dt, 1H,J1=2.8 Hz, J2=12 Hz); 2.32(s, 3H); 1.45(d, 3H, J=6.8 Hz); 1.33(s, 9H);

MS: 364.2(M+1).

The identity of Compound CTW wherein Q is (R)—CH₃ was confirmed using H¹NMR and mass spectrometry.

Compound CTW wherein Q is (R)—CH₃: ¹H NMR (CDCl₃), δ 8.49(d, 1H, J=4.8Hz); 7.93(dd, 1H, J1=1.6 Hz, J2=8.0 Hz); 7.42(s, 1H); 7.26(d, 1H, J=8.4Hz); 7.14(dd, 1H, J1=1.6 Hz, J2=8.4 Hz); 7.08(dd, 1H, J1=4.8 Hz, J2=8.0Hz); 4.37(m, 1H); 3.89(d, 1H, J=12 Hz); 3.64(dt, 1H, J1=3.2 Hz, J2=12Hz); 3.56(d, 1H, J=13 Hz); 3.45(d, 1H, J=13 Hz); 3.37(dd, 1H, J1=3.6 Hz,J2=12 Hz); 3.17(dt, 1H, J1=3.2 Hz, J2=12 Hz); 1.39(d, 3H, J=6.8 Hz);1.35(s, 9H).

MS: 418.2(M+1).

The identity of Compound CRW wherein Q is (R)—CH₃ was confirmed using H¹NMR and mass spectrometry.

Compound CRW wherein Q is (R)—CH₃: ¹H NMR (CD₃OD), δ 8.21(dd, 1H, J1=1.6Hz, J2=4.8 Hz); 7.78(dd, 1H, J1=1.6 Hz, J2=7.6 Hz); 7.24(s, 1H); 7.20(d,1H, J=8 Hz); 7.02(dd, 1H, J1=4.8 Hz, J2=8 Hz); 7.01(d, 1H, J=8 Hz);4.36(m, 1H); 3.86(m, 3H); 3.62(dt, 1H, J1=3.2 Hz, J2=12 Hz); 3.18(dd,1H, J1=2.8 Hz, J2=13 Hz); 3.07(dt, 1H, J1=3.2 Hz, J2=13 Hz); 1.46(d, 3H,J=6.8 Hz).

MS: 362.1(M+1).

The identity of Compound CSB wherein Q is (R)—CH₃ was confirmed using H¹NMR and mass spectrometry.

Compound CSB wherein Q is (R)—CH₃: ¹H NMR (CD₃OD), δ 8.24(dd, 1H, J1=1.8Hz, J2=4.8 Hz); 7.80(dd, 1H, J1=1.8 Hz, J2=7.9 Hz); 4.31(m, 1H); 3.91(m,2H); 3.80(dt, 1H, J1=3.5 Hz, J2=12 Hz); 3.25(dd, 1H, J1=3.2 Hz, J2=12Hz); 3.15(dt, 1H, J1=4.0 Hz, J2=12 Hz); 1.56(d, 3H, J=6.6 Hz).

MS: 358.1(M+1).

5.5. Example 5 Synthesis of Benzoazolylpiperazine Compound of Formula(IIb) DBM

Compound DBM wherein R₃ is (R)—CH₃ was prepared by a method analogous tothat used in Example 4 except that 4,5-dichlorothiadiazole was used inplace of 2-chloro-3-X-pyridine 1 and the 2-Q-piperazine 2 was2-(R)-methylpiperazine and the 5-Z-6-Y-2-chloro-1-H-benzoimidazole 7 was6-tert-butyl-2-chloro-1-H-benzoimidazole.

The identity of Compound DBM wherein Q is (R)—CH₃ was confirmed using H¹NMR and mass spectrometry.

Compound DBM wherein Q is (R)—CH₃: ¹H NMR (CD₃OD), δ 7.34(s, 1H);7.20(d, 1H, J=8.4 Hz); 7.13(dd, 1H, J1=1.6 Hz, J2=8.4 Hz); 4.38(m, 1H);4.05(bd, 2H, J=12 Hz); 3.90(bd, 1H, J=13 Hz); 3.58(dt, 1H, J1=3.6 Hz,J2=12 Hz); 3.27(dd, 1H, J1=3.6 Hz, J2=12 Hz); 3.20(dt, 1H, J1=3.6 Hz,J2=12 Hz); 1.43(d, 3H, J=6.4 Hz); 1.37(s, 9H).

MS: 391.1(M+1).

5.6. Example 6 Synthesis of Benzoazolylpiperazine Compound of Formula 10

Benzoazolylpiperazine compound of Formula 10

was prepared by a method analogous to that used in Example 4 usingcompound 7 wherein Y is —CH₃ and Z is —CH(CH₃)₂ and2-(R)-methylpiperazine for the 2-Q-piperazine 2.

The identity of Compound 10 wherein Q is (R)—CH₃ was confirmed using H¹NMR and mass spectrometry.

Compound 10 wherein Q is (R)—CH₃: ¹H NMR (CD₃OD), δ 8.22(dd, 1H, J1=1.8Hz, J2=4.9 Hz); 7.78(dd, 1H, J1=1.6 Hz, J2=8.0 z); 7.20(s, 1H); 7.04(dd,1H, J1=4.9 Hz, J2=7.7 Hz); 4.35(m, 1H); 3.85(m, 3H); 3.62(dt, 1H, J1=3.3Hz, J2=12 Hz); 3.21(m, 2H); 3.06(dt, 1H, J1=4.0 Hz, J2=13 Hz); 2.40(s,3H); 1.47(d, 3H, J=6.8 Hz); 1.27(d, 6H, J=6.8 Hz).

MS: 384.1(M+1).

5.7. Example 7 Synthesis of Benzoazolylpiperazine Compound of Formula(IIa) FUY and EXG

Compound 3 (about 1 mmol), prepared as described above in Example 5.1and 1 eq. of compound 11 were dissolved in toluene or p-xylene (about0.5 to about 1 mL) and the resulting reaction mixture was heated in asealed tube at a temperature of about 150° C. for about 24 h. Thereaction mixture was then concentrated under reduced pressure to providea residue. The resulting residue was purified using flash chromatography(silica gel, 5% methanol:DCM) to provide the BenzoazolylpiperazineCompounds of formula (IIIa).

Compound 11 was obtained as described below

Compound 12 (about 15 to about 20 mmol) and 1 eq. of compound 13, weredissolved in ethanol (about 30 to about 40 mL) and the resultingreaction mixture heated at reflux temperature for about 5 h. Thereaction mixture was then concentrated under reduced pressure to providea residue that was diluted with water (about 30 mL) and acidified withacetic acid to a pH value of about 6. The aqueous mixture was extractedwith ethyl acetate, the ethyl acetate dried (Na₂SO₄), and the solventremoved under reduced pressure to provide compound 7 that was usedwithout further purification.

Table XXV lists the Benzoazolylpiperazine Compounds that were preparedaccording to the method of Example 7.

TABLE XXV Benzoazolylpiperazine Compound Y Z X Q FUY —H tert-butyl —Cl(R)—CH₃ EXG —H tert-butyl —Cl —H (R)—CH₃ means that the carbon atom towhich the methyl group is attached is in the (R) configuration.

The identity of Compound FUY was confirmed using H¹ NMR and massspectrometry.

Compound FUY: ¹H NMR (CDCl₃), δ 8.23(dd, 1H, J1=1.6 Hz, J2=4.8 Hz);7.65(dd, 1H, J1=2 Hz, J2=7.6 Hz); 7.47(d, 1H, J=2 Hz); 7.20(d, 1H, J=8.4Hz); 7.10(dd, 1H, J1=2 Hz, J2=8.4 Hz); 6.91(dd, 1H, J1=4.8 Hz, J2=8 Hz);4.60(m, 1H); 4.60(d, 1H, J=13 Hz); 3.84(m, 2H); 3.67(dt, 1H, J1=3.6 Hz,J2=13 Hz); 3.17(dd, 1H, J1=4 Hz, J2=12 Hz); 3.08(dt(1H, J1=3.2 Hz, J2=12Hz); 1.52(d, 3H, J=6.8 Hz); 1.37(s, 9H).

MS: 385.2(M+1).

The identity of Compound EXG wherein Q is (R)—CH₃ was confirmed using H¹NMR and mass spectrometry.

Compound EXG: ¹H NMR (CDCl₃), δ 8.23(dd, 1H, J1=1.6 Hz, J2=4.8 Hz);7.65(dd, 1H, J1=2 Hz, J2=7.6 Hz); 7.46(d, 1H, J=1.6 Hz); 7.20(dd, 1H,J1=0.4 Hz, J2=8.4 Hz); 7.10(dd, 1H, J1=2 Hz, J2=8.4 Hz);6.91(dd, 1H,J1=5.2 Hz, J2=7.6 Hz); 3.88(m, 4H); 3.50(m, 4H); 1.37(s, 9H).

MS: 371.1(M+1).

5.8. Example 8 Synthesis of Benzoazolylpiperazine Compound of Formula(IIIa) FIU

Compound FIU was prepared by a method analogous to that used in Example1 except that 5-chloro-benzooxoazol-2-ylamine was used in place of the5-Z-6-Y-benzothiazol-2-ylamine.

The identity of Compound FIU was confirmed using H¹ NMR.

Compound FIU: ¹H NMR (CDCl₃), δ11.45 (bs, 1H), 8.23-8.18 (m, 1H),7.66-7.61 (m, 1H), 7.25-7.21 (m, 1H), 7.18-7.12 (m, 1H), 6.92-6.86 (m,1H), 5.06-4.71 (m, 1H), 4.67-4.32 (m, 1H), 3.87-3.72 (m, 2H), 3.56-3.29(m, 1H), 3.07-2.86 (m, 2H), 1.45 (d, 3H, J=6.8).

5.9. Example 9 Synthesis of Benzoazolylpiperazine Compound of Formula 14

2-Amino-6-methyl-benzothiazole 15 (2.0 mmol, 328 mg) (commerciallyavailable from Sigma-Aldrich, St. Louis, Mo. (www.sigma-aldrich.com))and 1,1′-thiocarbonyldiimidazole (2.0 mmol, 356 mg) (commerciallyavailable from Sigma-Aldrich, St. Louis, Mo. (www.sigma-aldrich.com))were suspended in DMSO (3 mL). 4-Dimethyl-aminopyridine (30 mg)(commercially available from Sigma-Aldrich, St. Louis, Mo.(www.sigma-aldrich.com)) was then added to the suspension and theresulting reaction mixture heated to 100° C. and stirred at 100° C. forabout 6 hours. The reaction mixture was then cooled to room temperatureand (R)-4-(3-chloro-2-pyridinyl)-2-methylpiperazine (2.0 mmol, 422 mg)(commercially available from Sigma-Aldrich, St. Louis, Mo.(www.sigma-aldrich.com)) was added to the reaction mixture. The reactionmixture was heated to 100° C. and stirred at 100° C. for 16 hours. Thesolvent was then removed under reduced pressure to provide a residuethat was purified using flash chromatography on a silica column elutedwith ethyl acetate/hexane (gradient elution from 20:80 ethylacetate/hexane to 10:90 ethyl acetate/hexane) to provide compound 14 asa yellow solid.

The identity of Compound 14 was confirmed using H¹ NMR.

Compound 14: ¹H NMR (CDCl₃), 8.21 (1H, dd, J=1.6, 4.7 Hz), 7.63 (1H, dd,J=1.6, 7.8 Hz), 7.40 (1H, d, J=0.5 Hz), 7.18 (2H, d, J=0.5 Hz), 6.89(1H, dd, J=4.7, 7.8 Hz), 5.62 (1H, br), 5.27 (m, 1H), 3.84 (2H, t,J=10.6 Hz), 3.50 (1H, dt, J=2.9, 15.3 Hz), 3.08 (1H, dd, J=3.6, 12.6Hz), 3.00 (1H, dt, J=3.3, 15.3 Hz), 2.44 (3H, s), 1.48 (3H, d, J=7.2 Hz)ppm.

(M+1) m/z: 418.0.

5.10. Example 10 Synthesis of Benzoazolylpiperazine Compound GIO

Compound 17 (5 g, 30.7 mmol) and piperazine 2 (3.1 g, 30.7 mmol) weredissolved in 18 mL of DMSO and stirred at 100° C. for about 3 h. Thereaction mixture was then cooled to room temperature and the solventremoved under reduced pressure to provide a mixture of compounds 18 and19.

A solution of 6-fluoro-benzothiazol-2-ylamine 20 (3.7 g, 23.0 mmol) inDCM (15 mL) was added portionwise to a cooled solution of chloroformate4. The resulting reaction mixture was stirred for 5 min. and 10 mL oftriethylamine was added to the solution. The reaction mixture was thenallowed to warm to room temperature and concentrated under reducedpressure at about 40° C. to provide the compound of formula 21. Thecompound of formula 21 was redissolved in DCM (30 mL) and to theresulting solution was added the mixture of compounds 18 and 19,prepared as described above, in DCM (10 mL). The resulting reactionmixture was allowed to stir for 5 min. and the solvent was removed underreduced pressure to provide a residue comprising Compound GIO and aBenzoazolylpiperazine Compound of Formula 22. The residue was purifiedusing a silica gel column eluted with 5:95 ethyl acetate: hexane toprovide 0.69 g of Compound GIO.

5.11. Example 11 Binding of Benzoazolylpiperazine Compounds to mGluR5

The following assay can be used to demonstrates BenzoazolylpiperazineCompounds that bind to and modulate the activity of mGluR5.

Cell cultures: Primary glial cultures are prepared from cortices ofSprague-Dawley 18 days old embryos. The cortices are dissected and thendissociated by trituration. The resulting cell homogenate is plated ontopoly-D-lysine precoated T175 flasks (BIOCOAT, commercially availablefrom Becton Dickinson and Company Inc. of Franklin Lakes, N.J. ) inDulbelcco's Modified Eagle's Medium (“DMEM,” pH 7.4), buffered with 25mM HEPES, and supplemented with 15% fetal calf serum (“FCS,”commercially available from Hyclone Laboratories Inc. of Omaha, Nebr. ),and incubated at 37° C. and 5% CO₂. After 24 hours, FCS supplementationis reduced to 10%. On day six, oligodendrocytes and microglia areremoved by strongly tapping the sides of the flasks. One day followingthis purification step, secondary astrocyte cultures are established bysubplating onto 96 poly-D-lysine precoated T175 flasks (BIOCOAT) at adensity of 65,000 cells/well in DMEM and 10% FCS. After 24 hours, theastrocytes are washed with serum free medium and then cultured in DMEM,without glutamate, supplemented with 0.5% FCS, 20 mM HEPES, 10 ng/mLepidermal growth factor (“EGF”), 1 mM sodium pyruvate, and 1×penicillin/streptomycin at pH 7.5 for 3 to 5 days at 37° C. and 5% CO₂The procedure allows the expression of the mGluR5 receptor byastrocytes, as demonstrated by S. Miller et al., J. Neuroscience15(9):6103-6109 (1995).

Assay Protocol: After 3-5 days incubation with EGF, the astrocytes arewashed with 127 mM NaCl, 5 mM KCl, 2 mM MgCl₂, 700 mM NaH₂PO₄, 2 mMCaCl₂, 5 mM NaHCO₃, 8 mM HEPES, 10 mM Glucose at pH 7.4 (“Assay Buffer”)and loaded with the dye Fluo-4 (commercially available from MolecularProbes Inc. of Eugene, Oreg.) using 0.1 mL of Assay Buffer containingFluo-4 (3 mM final). After 90 minutes of dye loading, the cells are thenwashed twice with 0.2 mL Assay Buffer and resuspended in 0.1 mL of AssayBuffer. The plates containing the astrocytes are then transferred to aFluorometric Imaging Plate reader (commercially available from MolecularDevices Corporation of Sunnyvale, Calif.) for the assessment of calciummobilization flux in the presence of glutamate and in the presence orabsence of antagonist. After monitoring fluorescence for 15 seconds toestablish a base line, DMSO solutions containing various concentrationsof a Benzoazolylpiperazine Compound diluted in Assay Buffer (0.05 mL of4× dilutions for competition curves) are added to the cell plate andfluorescence is monitored for 2 minutes. 0.05 mL of a 4× glutamatesolution (agonist) is then added to each well to provide a finalglutamate concentration in each well of 10 mM. Plate fluorescence isthen monitored for an additional 60 seconds after agonist addition. Thefinal DMSO concentration in the assay is 1.0%. In each experiment,fluorescence is monitored as a function of time and the data analyzedusing Microsoft Excel and GraphPad Prism. Dose-response curves are fitusing a non-linear regression to determine IC₅₀ value. In eachexperiment, each data point is determined two times. The assay resultswill demonstrate Benzoazolylpiperazine Compounds that bind to andmodulate the activity of mGluR5.

5.12. Example 12 In Vivo Assays for Prevention or Treatment of Pain

Test Animals: Each experiment uses rats weighing between 200-260 g atthe start of the experiment. The rats are group-housed and have freeaccess to food and water at all times, except prior to oraladministration of a Benzoazolylpiperazine Compound when food is removedfor 16 hours before dosing. A control group acts as a comparison to ratstreated with a Benzoazolylpiperazine Compound. The control group isadministered the carrier for the Benzoazolylpiperazine Compound. Thevolume of carrier administered to the control group is the same as thevolume of carrier and Benzoazolylpiperazine Compound administered to thetest group.

Acute Pain: To assess the actions of the Benzoazolylpiperazine Compoundsfor the treatment or prevention of acute pain the rat tail flick testcan be used. Rats are placed inside a cotton pouch and the tail exposedto a focused beam of radiant heat at a point 3 cm from the tip using atail flick unit (Model 7360, commercially available from Ugo Basile ofItaly). Tail flick latencies are defined as the interval between theonset of the thermal stimulus and the flick of the tail. Animals notresponding within 15 seconds are removed from the tail flick unit andassigned a withdrawal latency of 15 seconds. Tail flick latencies aremeasured immediately before (pre-treatment) and 1, 3, and 6 hoursfollowing administration of a Benzoazolylpiperazine Compound. Data areexpressed as tail flick latency(s) and the percentage of the maximalpossible effect (% MPE), i.e., 15 seconds, is calculated as follows:

${\%\mspace{14mu}{MPE}} = {\frac{\begin{matrix}\left\lbrack {\left( {{post}\mspace{14mu}{administration}\mspace{14mu}{latency}} \right) -} \right. \\\left. \left( {{pre}\text{-}{administration}\mspace{14mu}{latency}} \right) \right\rbrack\end{matrix}}{\left. {15\mspace{14mu} s\mspace{14mu}{pre}\text{-}{administration}\mspace{14mu}{latency}} \right)} \times 100}$The rat tail flick test is described in F. E. D'Amour et al., “A Methodfor Determining Loss of Pain Sensation,” J Pharmacol. Exp. Ther.72:74-79 (1941). The results will demonstrate BenzoazolylpiperazineCompounds that are useful for treating or preventing acute pain.

Acute pain can also be assessed by measuring the animal's response tonoxious mechanical stimuli by determining the paw withdrawal threshold(PWT), as described below.

Inflammatory Pain: To assess the actions of the BenzoazolylpiperazineCompounds for the treatment or prevention of inflammatory pain theFreund's complete adjuvant (FCA) model of inflammatory pain is used.FCA-induced inflammation of the rat hind paw is associated with thedevelopment of persistent inflammatory mechanical hyperalgesia andprovides reliable prediction of the anti-hyperalgesic action ofclinically useful analgesic drugs (L. Bartho et al., “Involvement ofCapsaicin-sensitive Neurones in Hyperalgesia and Enhanced OpioidAntinociception in Inflammation,” Naunyn-Schmiedeberg's Archives ofPharmacology 342:666-670 (1990)). The left hind paw of each animal isadministered a 50 μL intraplantar injection of 100% FCA. 24 hour postinjection, the animal is assessed for response to noxious mechanicalstimuli by determining the PWT, as described below. Rats are thenadministered a single injection of 1, 3, 10 or 30 mg/Kg of either aBenzoazolylpiperazine Compound, 30 mg/Kg indomethacin or carrier.Responses to noxious mechanical stimuli are then determined 2, 4, 6, and24 hours post administration. Percentage reversal of hyperalgesia foreach animal is defined as:

${\%\mspace{14mu}{Revesal}} = {\frac{\begin{matrix}\left\lbrack {\left( {{post}\mspace{14mu}{administration}\mspace{14mu}{PWT}} \right) -} \right. \\\left. \left( {{pre}\text{-}{administration}\mspace{14mu}{PWT}} \right) \right\rbrack\end{matrix}}{\left( {{Baseline}\mspace{14mu}{pre}\text{-}{administration}\mspace{14mu}{PWT}} \right)} \times 100}$The results will demonstrate Benzoazolylpiperazine Compounds that areuseful for treating or preventing inflammatory pain.

Neuropathic Pain: To assess the actions of the BenzoazolylpiperazineCompounds for the treatment or prevention of neuropathic pain either theSeltzer model or the Chung model can be used.

In the Seltzer model, the partial sciatic nerve ligation model ofneuropathic pain is used to produce neuropathic hyperalgesia in rats (Z.Seltzer et al., “A Novel Behavioral Model of Neuropathic Pain DisordersProduced in Rats by Partial Sciatic Nerve Injury,” Pain 43:205-218(1990)). Partial ligation of the left sciatic nerve is performed underenflurane/O₂ inhalation anaesthesia. Following induction of anesthesia,the left thigh of the rat is shaved and the sciatic nerve exposed athigh thigh level through a small incision and is carefully cleared ofsurrounding connective tissues at a site near the trocanther just distalto the point at which the posterior biceps semitendinosus nerve branchesoff of the common sciatic nerve. A 7-0 silk suture is inserted into thenerve with a ⅜ curved, reversed-cutting mini-needle and tightly ligatedso that the dorsal ⅓ to ½ of the nerve thickness is held within theligature. The wound is closed with a single muscle suture (7-0 silk) anda Michelle clip. Following surgery, the wound area is dusted withantibiotic powder. Sham-treated rats undergo an identical surgicalprocedure except that the sciatic nerve is not manipulated. Followingsurgery, animals are weighed and placed on a warm pad until they recoverfrom anesthesia. Animals are then returned to their home cages untilbehavioral testing begins. The animal is assessed for response tonoxious mechanical stimuli by determining PWT, as described below,immediately prior to and 1, 3, and 6 hours after drug administration forboth the left rear paw and right rear paw of the animal. Percentagereversal of neuropathic hyperalgesia is defined as:% reversal=100×[(right pre-administration PWT−left post-administrationPWT)/(right pre-administration PWT−left pre-administration PWT)]×100.

In the Chung model, the spinal nerve ligation model of neuropathic painis used to produce mechanical hyperalgesia, themal hyperalgesia andtactile allodynia in rats. Surgery is performed under isoflurane/O₂inhalation anaesthesia. Following induction of anaesthesia a 3 cmincision is made and the left paraspinal muscles are separated from thespinous process at the L₄-S₂ levels. The L₆ transverse process iscarefully removed with a pair of small rongeurs to identify visually theL₄-L₆ spinal nerves. The left L₅ (or L₅ and L₆) spinal nerve(s) isisolated and tightly ligated with silk thread. A complete hemostasis isconfirmed and the wound is sutured using non-absorbable sutures, such asnylon sutures or stainless steel staples. Sham-treated rats undergo anidentical surgical procedure except that the spinal nerve(s) is notmanipulated. Following surgery animals are weighed, administered asubcutaneous (s.c.) injection of saline or ringers lactate, the woundarea is dusted with antibiotic powder and they are kept on a warm paduntil they recover from the anesthesia. Animals are then be returned totheir home cages until behavioral testing begins. The animals areassessed for response to noxious mechanical stimuli by determining PWT,as described below, immediately prior to and 1, 3, and 5 hours afterbeing administered a Benzoazolylpiperazine Compound for both the leftrear paw and right rear paw of the animal. The animal can also beassessed for response to noxious thermal stimuli or for tactileallodynia, as described below. The Chung model for neuropathic pain isdescribed in S. H. Kim, “An Experimental Model for Peripheral NeuropathyProduced by Segmental Spinal Nerve Ligation in the Rat,” Pain50(3):355-363 (1992). The results show demonstrate BenzoazolylpiperazineCompounds that are useful for treating or preventing neuropathic pain.

Response to Mechanical Stimuli as an Assessment of MechanicalHyperalgesia: The paw pressure assay can be used to assess mechanicalhyperalgesia. For this assay, hind paw withdrawal thresholds (PWT) to anoxious mechanical stimulus are determined using an analgesymeter (Model7200, commercially available from Ugo Basile of Italy) as described inC. Stein, “Unilateral Inflammation of the Hindpaw in Rats as a Model ofProlonged Noxious Stimulation: Alterations in Behavior and NociceptiveThresholds,” Pharmacology Biochemistry and Behavior 31:451-455 (1988).The maximum weight that can be applied to the hind paw is set at 250 gand the end point is taken as complete withdrawal of the paw. PWT isdetermined once for each rat at each time point and only the affected(ipsilateral) paw is tested.

Response to Thermal Stimuli as an Assessment of Thermal Hyperalgesia:The plantar test can be used to assess thermal hyperalgesia. For thistest, hind paw withdrawal latencies to a noxious thermal stimulus aredetermined using a plantar test apparatus (commercially available fromUgo Basile of Italy) following the technique described by K. Hargreaveset al., “A New and Sensitive Method for Measuring Thermal Nociception inCutaneous Hyperalgesia,” Pain 32(1):77-88 (1988). The maximum exposuretime is set at 32 seconds to avoid tissue damage and any directed pawwithdrawal from the heat source is taken as the end point. Threelatencies are determined at each time point and averaged. Only theaffected (ipsilateral) paw is tested.

Assessment of Tactile Allodvnia: To assess tactile allodynia, rats areplaced in clear, plexiglass compartments with a wire mesh floor andallowed to habituate for a period of at least 15 minutes. Afterhabituation, a series of von Frey monofilaments are presented to theplantar surface of the left (operated) foot of each rat. The series ofvon Frey monofilaments consists of six monofilaments of increasingdiameter, with the smallest diameter fiber presented first. Five trialsare conducted with each filament with each trial separated byapproximately 2 minutes. Each presentation lasts for a period of 4-8seconds or until a nociceptive withdrawal behavior is observed.Flinching, paw withdrawal or licking of the paw are considerednociceptive behavioral responses.

5.13 Example 13 In Vivo Assays for Prevention or Treatment of Anxiety

The elevated plus maze test or the shock-probe burying test can be usedto assess the anxiolytic activity of Benzoazolylpiperazine Compounds inrats or mice.

The Elevated Plus Maze Test: The elevated plus maze consists of aplatform with 4 arms, two open and two closed (50×10×50 cm enclosed withan open roof). Rats (or mice) are placed in the center of the platform,at the crossroad of the 4 arms, facing one of the closed arms. Timespent in the open arms vs the closed arms and number of open arm entriesduring the testing period are recorded. This test is conducted prior todrug administration and again after drug administration. Test resultsare expressed as the mean time spent in open arms and the mean number ofentries into open arms. Known anxiolytic drugs increase both the timespent in open arms and number of open arm entries. The elevated plusmaze test is described in D. Treit, “Animal Models for the Study ofAnti-anxiety Agents: A Review,” Neuroscience & Biobehavioral Reviews9(2):203-222 (1985).

The Shock-Probe Burying Test: For the shock-probe burying test thetesting apparatus consists of a plexiglass box measuring 40×30×40 cm,evenly covered with approximately 5 cm of bedding material (odorabsorbent kitty litter) with a small hole in one end through which ashock probe (6.5 cm long and 0.5 cm in diameter) is inserted. Theplexiglass shock probe is helically wrapped with two copper wiresthrough which an electric current is administered. The current is set at2 mA. Rats are habituated to the testing apparatus for 30 min on 4consecutive days without the shock probe in the box. On test day, ratsare placed in one corner of the test chamber following drugadministration. The probe is not electrified until the rat touches itwith its snout or fore paws, at which point the rat receives a brief 2mA shock. The 15 min testing period begins once the rat receives itsfirst shock and the probe remains electrified for the remainder of thetesting period. The shock elicits burying behavior by the rat. Followingthe first shock, the duration of time the rat spends spraying beddingmaterial toward or over the probe with its snout or fore paws (buryingbehavior) is measured as well as the number of contact-induced shocksthe rat receives from the probe. Known anxiolytic drugs reduce theamount of burying behavior. In addition, an index of the rat'sreactivity to each shock is scored on a 4 point scale. The total timespent immobile during the 15 min testing period is used as an index ofgeneral activity. The shock-probe burying test is described in D. Treit,1985, supra. The results of this test will demonstrateBenzoazolylpiperazine Compounds that are useful for treating orpreventing anxiety.

5.14. Example 14 In Vivo Assays for Prevention or Treatment of anAddictive Disorder

The condition place preference test or drug self-administration test canbe used to assess the ability of Benzoazolylpiperazine Compounds toattenuate the rewarding properties of known drugs of abuse.

The Condition Place Preference Test: The apparatus for the conditionedplace preference test consists of two large compartments (45×45×30 cm)made of wood with a plexiglass front wall. These two large compartmentsare distinctly different. Doors at the back of each large compartmentlead to a smaller box (36×18×20 cm) box made of wood, painted grey, witha ceiling of wire mesh. The two large compartments differ in terms ofshading (white vs black), level of illumination (the plexiglass door ofthe white compartment is covered with aluminum foil except for a windowof 7×7 cm), texture (the white compartment has a 3 cm thick floor board(40×40 cm) with nine equally spaced 5 cm diameter holes and the blackhas a wire mesh floor), and olfactory cues (saline in the whitecompartment and 1 mL of 10% acetic acid in the black compartment). Onhabituation and testing days, the doors to the small box remain open,giving the rat free access to both large compartments.

The first session that a rat is placed in the apparatus is a habituationsession and entrances to the smaller grey compartment remain open givingthe rat free access to both large compartments. During habituation, ratsgenerally show no preference for either compartment. Followinghabituation, rats are given 6 conditioning sessions. Rats are dividedinto 4 groups: carrier pre-treatment+carrier (control group),2-Pyrimidinylpiperazine Compound pre-treatment+carrier, carrierpre-treatment+morphine, 2-Pyrimidinylpiperazine Compoundpre-treatment+morphine. During each conditioning session the rat isinjected with one of the drug combinations and confined to onecompartment for 30 min. On the following day, the rat receives acarrier+carrier treatment and is confined to the other largecompartment. Each rat receives three conditioning sessions consisting of3 drug combination-compartment and 3 carrier-compartment pairings. Theorder of injections and the drug/compartment pairings arecounterbalanced within groups. On the test day, rats are injected priorto testing (30 min to 1 hour) with either morphine or carrier and therat is placed in the apparatus, the doors to the grey compartment remainopen and the rat is allowed to explore the entire apparatus for 20 min.The time spent in each compartment is recorded. Known drugs of abuseincrease the time spent in the drug-paired compartment during thetesting session. If the Benzoazolylpiperazine Compound blocks theacquisition of morphine conditioned place preference (reward), therewill be no difference in time spent in each side in rats pre-treatedwith a Benzoazolylpiperazine Compound and the group will not bedifferent from the group of rats that was given carrier+carrier in bothcompartments. Data will be analyzed as time spent in each compartment(drug combination-paired vs carrier-paired). Generally, the experimentis repeated with a minimum of 3 doses of a BenzoazolylpiperazineCompound.

The Drug Self-Administration Test: The apparatus for the drugself-administration test is a standard commercially available operantconditioning chamber. Before drug trials begin rats are trained to pressa lever for a food reward. After stable lever pressing behavior isacquired, rats are tested for acquisition of lever pressing for drugreward. Rats are implanted with chronically indwelling jugular cathetersfor i.v. administration of compounds and are allowed to recover for 7days before training begins. Experimental sessions are conducted dailyfor 5 days in 3 hour sessions. Rats are trained to self-administer aknown drug of abuse, such as morphine. Rats are then presented with twolevers, an “active” lever and an “inactive” lever. Pressing of theactive lever results in drug infusion on a fixed ratio 1 (FR1) schedule(i.e., one lever press gives an infusion) followed by a 20 second timeout period (signaled by illumination of a light above the levers).Pressing of the inactive lever results in infusion of excipient.Training continues until the total number of morphine infusionsstabilizes to within ±10% per session. Trained rats are then used toevaluate the effect of Benzoazolylpiperazine Compounds pre-treatment ondrug self-administration. On test day, rats are pre-treated with aBenzoazolylpiperazine Compound or excipient and then are allowed toself-administer drug as usual. If the Benzoazolylpiperazine Compoundblocks the rewarding effects of morphine, rats pre-treated with theBenzoazolylpiperazine Compound will show a lower rate of respondingcompared to their previous rate of responding and compared to excipientpre-treated rats. Data is analyzed as the change in number of druginfusions per testing session (number of infusions during testsession−number of infusions during training session). The results willdemonstrate Benzoazolylpiperazine Compounds are useful for treating orpreventing an addictive disorder.

5.15. Example 15 Functional Assay for Characterizing mGluR 1Antagonistic Properties

Functional assays for the characterization of mGluR 1 antagonisticproperties are well known in the art. For example, the followingprocedure can be used.

A CHO-rat mGluR1 cell line is generated using cDNA encoding rat mGluR1receptor (M. Masu and S. Nakanishi, Nature 349: 760-765 (1991)). ThecDNA encoding rat mGluR1 receptor can be obtained from, e.g., Prof. S.Nakanishi (Kyoto, Japan).

40,000 CHO-rat mGluR1 cells/well are plated into a Costar 3409, black,clear bottom, 96 well, tissue culture treated plate (commerciallyavailable from Fisher Scientific of Chicago, Ill.) and are incubated inDulbecco's Modified Eagle's Medium (DMEM, pH 7.4) supplemented withglutamine, 10% FBS, 1% Pen/Strep, and 500 μg/mL Geneticin for about 12h. The CHO-rat mGluR1 cells are then washed and treated with Optimemmedium (commercially available from Invitrogen, Carlsbad, Calif.) andincubated for a time period ranging from 1 to 4 hours prior to loadingthe cells with the dye Fluo-4 (commercially available from MolecularProbes Inc., Eugene Oreg.). After incubation, the cell plates are washedwith loading buffer (127 mM NaCl, 5 mM KCl, 2 mM MgCl₂, 700 μM, NaH₂PO₄,2 mM CaCl₂, 5 mMNaHCO₃, 8 mM HEPES, and 10 mM glucose, pH 7.4) andincubated with 3 μM Fluo-4 in 0.1 mL loading buffer for 90 min. Thecells are then washed twice with 0.2 mL loading buffer, resuspended in0.1 mL of loading buffer, and transferred to a Fluorometric ImagingPlate Reader (FLIPR) (commercially available from Molecular DevicesCorp., Sunnyvale, Calif.) for measurement of calcium mobilization fluxin the presence of glutamate and in the presence or absence of aBenzoazolylpiperazine Compound.

To measure calcium mobilization flux, fluoresence is monitored for about15 s to establish a baseline and DMSO solutions containing variousconcentrations of a Benzoazolylpiperazine Compound ranging from about 50μM to about 0.8 nM diluted in loading buffer (0.05 mL of a 4× dilution)are added to the cell plate and fluoresence is monitored for about 2min. 0.05 mL of a 4× Glutamate solution (agonist) is then added to eachwell to provide a final glutamate concentration in each well of 10 μMand fluoresence is monitored for about 1 additional min. The final DMSOconcentration in the assay is 1%. In each experiment fluoresence ismonitored as a function of time and the data is analyzed using anon-linear regression to determine the IC₅₀ value. In each experimenteach data point is determined twice.

5.16 Example 16 Binding of Benzoazolylpiperazine Compounds to VR1

Methods for demonstrating a compound's ability to inhibit VR1 are wellknown to those skilled in the art, for example, those methods disclosedin U.S. Pat. No. 6,239,267 to Duckworth et al.; U.S. Pat. No. 6,406,908to McIntyre et al.; or U.S. Pat. No. 6,335,180 to Julius et al. Theresults of this assay will demonstrate Benzoazolylpiperazine Compoundsthat bind to and modulate the activity of VR1.

Binding of Compound AAQ to VR1: Assay Protocol

Human VR1 cloning. Human spinal cord RNA (commercially available fromClontech, Palo Alto, Calif.) was used. Reverse transcription wasconducted on 1.0 μg total RNA using Thermoscript Reverse Transcriptase(commercially available from Invitrogen, Carlsbad, Calif.) and oligo dTprimers as detailed in its product description. Reverse transcriptionreactions were incubated at 55° C. for 1 h, heat-inactivated at 85° C.for 5 min, and RNase H-treated at 37° C. for 20 min.

Human VR1 cDNA sequence was obtained by comparison of the human genomicsequence, prior to annotation, to the published rat sequence. Intronsequences were removed and flanking exonic sequences were joined togenerate the hypothetical human cDNA. Primers flanking the coding regionof human VR1 were designed as follows: forward primer,AAGATCTTCGCTGGTTGCACACTGGGCCACA; and reverse primer,GAAGATCTTCGGGGACAGTGACGGTTGGATGT.

PCR of VR1 was performed on one tenth of the reverse transcriptionreaction mixture using Expand Long Template Polymerase and Expand Buffer2 in a final volume of 50 μL according to the manufacturer'sinstructions (Roche Applied Sciences, Indianapolis, Ind.). Afterdenaturation at 94° C. for 2 min PCR amplification was performed for 25cycles at 94° C. for 15 sec, 58° C. for 30 sec, and 68° C. for 3 minfollowed by a final incubation at 72° C. for 7 min to complete theamplification. A PCR product of ˜2.8 kb was gel-isolated using a 1.0%agarose, Tris-Acetate gel containing 1.6 μg/ML of crystal violet andpurified with a S.N.A.P. UV-Free Gel Purification Kit (commerciallyavailable from Invitrogen). The VR1 PCR product was cloned into thepIND/V5-His-TOPO vector (commercially available from Invitrogen)according to the manufacturer's instructions. DNA preparations,restriction enzyme digestions, and preliminary DNA sequencing wereperformed according to standard protocols. Full-length sequencingconfirmed the identity of the human VR1.

Generation of inducible cell lines. Unless noted otherwise, cell culturereagents were purchased from Life Technologies of Rockville, Md.HEK293-EcR cells expressing the ecdysone receptor (commerciallyavailable from Invitrogen) were cultured in Growth Medium (Dulbecco'sModified Eagles Medium containing 10% fetal bovine serum (commerciallyavailable from HYCLONE, Logan, Utah), 1× penicillin/streptomycin, 1×glutamine, 1 mM sodium pyruvate and 400 μg/mL Zeocin (commerciallyavailable from Invitrogen)). The VR1-pIND constructs were transfectedinto the HEK293-EcR cell line using Fugene transfection reagent(commercially available from Roche Applied Sciences, Basel,Switzerland). After 48 h, cells were transferred to Selection Medium(Growth Medium containing 300 μg/mL G418 (commercially available fromInvitrogen)). Approximately 3 weeks later individual Zeocin/G418resistant colonies were isolated and expanded. To identify functionalclones, multiple colonies were plated into 96-well plates and expressionwas induced for 48 h using Selection Medium supplemented with 5 μMponasterone A (“PonA”) (commercially available from Invitrogen). On theday of assay, cells were loaded with Fluo-4 (a calcium-sensitive dyethat is commercially available from Molecular Probes, Eugene, Oreg.) andCAP-mediated calcium influx was measured using a Fluorometric ImagingPlate Reader (“FLIPR”) (commercially available from Molecular DevicesCorp., Sunnyvale, Calif.) as described below. Functional clones werere-assayed, expanded, and cryopreserved.

pH-Based Assay. Two days prior to performing this assay, cells wereseeded on poly-D-lysine-coated 96-well clear-bottom black plates(commercially available from Becton-Dickinson) at 75,000 cells/well ingrowth media containing 5 μM PonA (commercially available fromInvitrogen) to induce expression. On the day of the assay, the plateswere washed with 0.2 mL 1×Hank's Balanced Salt Solution (commerciallyavailable from Life Technologies) containing 1.6 mM CaCl₂ and 20 mMHEPES, pH 7.4 (“wash buffer”), and loaded using 0.1 mL of wash buffercontaining Fluo-4 (3 μM final concentration, commercially available fromMolecular Probes). After 1 h, the cells were washed twice with 0.2 mLwash buffer and resuspended in 0.05 mL 1× Hank's Balanced Salt Solution(commercially available from Life Technologies) containing 3.5 mM CaCl₂and 10 mM Citrate, pH 7.4 (“assay buffer”). Plates were then transferredto a FLIPR (commercially available from Molecular Devices) for assay.Compound AAQ was diluted in assay buffer, and 50 mL of the resultantsolution were added to the cell plates and the solution monitored fortwo minutes. The final concentration of Compound AAQ ranged from about50 pM to about 3 μM. Agonist buffer (wash buffer titrated with 1N HCl toprovide a solution having a pH of 5.5 when mixed 1:1 with assay buffer)(0.1 mL) was then added to each well, and the plates were incubated for1 additional min. Data were collected over the entire time course andanalyzed using Excel and Graph Pad Prism. Compound AAQ when assayedaccording to this protocol had an IC₅₀ of 261.8±75.1 (n=6).

Capsaicin-based Assay. Two days prior to performing this assay, cellswere seeded in poly-D-lysine-coated 96-well clear-bottom black plates(50,000 cells/well) in growth media containing 5 μM PonA (commerciallyavailable from Invitrogen) to induce expression. On the day of theassay, the plates were washed with 0.2 mL 1× Hank's Balanced SaltSolution (commercially available from Life Technologies) containing 1 mMCaCl₂ and 20 mM HEPES, pH 7.4, and cells were loaded using 0.1 mL ofwash buffer containing Fluo-4 (3 μM final). After one h, the cells werewashed twice with 0.2 mL of wash buffer and resuspended in 0.1 mL ofwash buffer. The plates were transferred to a FLIPR (commerciallyavailable from Molecular Devices) for assay. 50 μL of Compound AAQdiluted with assay buffer were added to the cell plates and incubatedfor 2 min. The final concentration of Compound AAQ ranged from about 50pM to about 3 μM. Human VR1 was activated by the addition of 50 μL ofcapsaicin (400 nM), and the plates were incubated for an additional 3min. Data were collected over the entire time course and analyzed usingExcel and GraphPad Prism. Compound AAQ when assayed according to thisprotocol had an IC₅₀ of 50.7±14.7 (n=3).

The results of the pH-based assay and the capsaicin-based assaydemonstrate that Compound AAQ, an illustrative BenzoazolylpiperazineCompound, binds to and modulates the activity of human VR1 and,accordingly, is useful for treating or preventing pain, UI, an ulcer,IBD, or IBS.

The present invention is not to be limited in scope by the specificembodiments disclosed in the examples which are intended asillustrations of a few aspects of the invention and any embodiments thatare functionally equivalent are within the scope of this invention.Indeed, various modifications of the invention in addition to thoseshown and described herein will become apparent to those skilled in theart and are intended to fall within the scope of the appended claims.

A number of references have been cited, the entire disclosures of whichare incorporated herein by reference.

1. A compound of formula:

or a pharmaceutically acceptable salt thereon wherein Ar₁ is

A is

R₁ is —Cl, —Br, —I, —(C₁-C₆)alkyl, —NO₂, —CN, —OH, —OCH₃, —NH₂,—C(halo)₃, —CH(halo)₂, or —CH₂(halo); each R₂ is independently: (a)-halo, —CN, —OH, —O(C₁-C₆)alkyl, —NO₂, or —NH₂; (b) —(C₁-C₁₀)alkyl,—(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl,—(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,—(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, eachof which is unsubstituted or substituted with one or more R₅ groups; or(c) -phenyl, -naphthyl, —(C₁₄)aryl, or -(5- to 10-membered)heteroaryl,each of which is unsubstituted or substituted with one or more R₆groups; each R₃ is independently: (a) -halo, —CN, —OH, —O(C₁-C₆)alkyl,—NO₂, or —NH₂; (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,—(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl,—(C₅-C₁₀)cycloalkenyl, —(C₈-C₁₄)bicycloalkenyl,—(C₈-C₁₄)tricycloalkenyl, -(3- to 7-membered)heterocycle, or -(7- to10-membered)bicycloheterocycle, each of which is unsubstituted orsubstituted with one or more R₅ groups; or (c) -phenyl, -naphthyl,—(C₁₄)aryl or -(5- to 10-membered)heteroaryl, each of which isunsubstituted or substituted with one or more R₆ groups; R₄ is —H or—(C₁-C₆)alkyl; each R₅ is independently —CN, —OH, -halo, —N₃, —NO₂,—N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇,—SR₇, —S(O)R₇, or —S(O)₂R₇; each R₆ is independently —(C₁-C₆)alkyl,—(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,—(C₅-C₈)cycloalkenyl, -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃,—CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇,—NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or—S(O)₂R₇; each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—(C₃-C₅)heterocycle, —C(halo)₃, —CH₂(halo), or —CH(halo)₂; R₈ and R₉ areeach independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl,—(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃,—CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —N(R₇)₂, —CH═NR₇, —NR₇OH,—OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;each -halo is —F, —Cl, —Br, or —I; n is an integer ranging from 0 to 3;m is 0 or 1; and x is 0 or
 1. 2. The compound of claim 1, wherein x is 1and A is —C(O)N(R₄)—.
 3. The compound of claim 1, wherein x is 1, and Ais —C(S)N(R₄)—.
 4. The compound of claim 1, wherein n is
 0. 5. Thecompound of claim 1, wherein n is
 1. 6. The compound of claim 1, whereinx is
 0. 7. The compound of claim 1, wherein: R₁ is —CH₃, —CF₃, —Cl, —Br,or —I; m is 0; n is 0; x is 1; A is —C(O)—N(R₄)—; R₄ is —H; R₈ is —H;and R₉ is —CH₃, —CF₃, —OCH₂CH₃, tert-butyl, —Cl, —Br, or —F.
 8. Thecompound of claim 7, wherein R₁ is —CH₃ and R₉ is —Cl.
 9. The compoundof claim 7, wherein R₁ is —CH₃ and R₉ is —Br.
 10. The compound of claim7, wherein R₁ is —CH₃ and R₉ is —F.
 11. The compound of claim 7, whereinR₁ is —Cl and R₉ is —Cl.
 12. The compound of claim 7, wherein R₁ is —Cland R₉ is —Br.
 13. The compound of claim 7, wherein R₁ is —Cl and R₉ is—F.
 14. The compound of claim 1, wherein: R₁ is —CH₃, —CF₃, —Cl, —Br, or—I; m is 1; R₃ is —(C₁-C₁₀)alkyl; n is 0; x is 1; A is —C(O)—N(R₄)—; R₄is —H; R₈ is —H; and R₉ is —CH₃, —CF₃, —OCH₂CH₃, tert-butyl, —Cl, —Br,or —F.
 15. The compound of claim 14, wherein R₃ is —CH₃.
 16. Thecompound of claim 14, wherein the carbon to which R₃ is attached is inthe (R) configuration.
 17. The compound of claim 14, wherein R₃ isattached to a carbon atom adjacent to a nitrogen atom attached to the—C(O)—N(R₄)-group.
 18. The compound of claim 14, wherein R₁ is —CH₃ andR₉ is —Cl.
 19. The compound of claim 18, wherein the carbon to which R₃is attached is in the (R) configuration.
 20. The compound of claim 14,wherein R₁ is —CH₃ and R₉ is —Br.
 21. The compound of claim 20, whereinthe carbon to which R₃ is attached is in the (R) configuration.
 22. Thecompound of claim 14, wherein R₁ is —CH₃ and R₉ is —F.
 23. The compoundof claim 22, wherein the carbon to which R₃ is attached is in the (R)configuration.
 24. The compound of claim 14, wherein R₁ is —Cl and R₉ is—Cl.
 25. The compound of claim 24, wherein the carbon to which R₃ isattached is in the (R) configuration.
 26. The compound of claim 14,wherein R₁ is —Cl and R₉ is —Br.
 27. The compound of claim 26, whereinthe carbon to which R₃ is attached is in the (R) configuration.
 28. Thecompound of claim 14, wherein R₁ is —Cl and R₉ is —F.
 29. The compoundof claim 28, wherein the carbon to which R₃ is attached is in the (R)configuration.
 30. The compound of claim 1, wherein m is 1 and thecarbon to which R₃ is attached is in the (R) configuration.
 31. Acompound of formula:

or a pharmaceutically acceptable salt thereof, wherein Ar₁ is

R₁ is —Cl, —Br, —I, —(C₁-C₆)alkyl, —NO₂, —CN, —OH, —OCH₃, —NH₂,—C(halo)₃, —CH(halo)₂, or —CH₂(halo); each R₂ is independently: (a)-halo, —CN, —OH, —O(C₁-C₆)alkyl, —NO₂, or —NH₂; (b) —(C₁-C₁₀)alkyl,—(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl,—(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,—(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, eachof which is unsubstituted or substituted with one or more R₅ groups; or(c) -phenyl, -naphthyl, —(C₁₄)aryl, or -(5- to 10-membered)heteroaryl,each of which is unsubstituted or substituted with one or more R₆groups; each R₃ is independently: (a) -halo, —CN, —OH, —O(C₁-C₆)alkyl,—NO₂, or —NH₂; (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,—(C₃-C₁₃)cycloalkyl, —(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl,—(C₅-C₁₀)cycloalkenyl, —(C₈-C₁₄)bicycloalkenyl,—(C₈-C₁₄)tricycloalkenyl, -(3- to 7-membered)heterocycle, or -(7- to10-membered)bicycloheterocycle, each of which is unsubstituted orsubstituted with one or more R₅ groups; or (c) -phenyl, -naphthyl,—(C₁₄)aryl or -(5- to 10-membered)heteroaryl, each of which isunsubstituted or substituted with one or more R₆ groups; each R₅ isindependently —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH,—OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;each R₆ is independently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—(C₃-C₅)heterocycle, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH, -halo,—N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇,—OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇; each R₇ is independently —H,—(C₁-C₆)alkyl, —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,—(C₅-C₈)cycloalkenyl, -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃,—CH₂(halo), or —CH(halo)₂; R₈ and R₉ are each independently —H,—(C₁-C₆)alkyl, —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,—(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN,—OH, -halo, —N₃, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,—OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇; R₁₀ is —(C₁-C₄)alkyl;each -halo is —F, —Cl, —Br, or —I; n is an integer ranging from 0 to 3;and m is 0 or
 1. 32. The compound of claim 31, wherein n is
 0. 33. Thecompound of claim 31, wherein n is
 1. 34. The compound of claim 31,wherein: R₁ is —OH₃, —CF₃, —Cl, —Br, or —I; m is 0; n is 0; R₈ is —H;and R₉ is —CH₃, —CF₃, —OCH₂CH₃, tert-butyl, —Cl, —Br, or —F.
 35. Thecompound of claim 31, wherein: R₁ is —CH₃, —CF₃, —Cl, —Br, or —I; m is1; R₃ is —(C₁-C₁₀)alkyl; n is 0; R₈ is —H; and R₉ is —CH₃, —CF₃,—OCH₂CH₃, tert-butyl, —Cl, —Br, or —F.
 36. The compound of claim 35,wherein R₃ is —CH₃.
 37. The compound of claim 35, wherein the carbon towhich R₃ is attached is in the (R) configuration.
 38. The compound ofclaim 31, wherein the carbon to which R₃ is attached is in the (R)configuration.
 39. A compound of formula:

or a pharmaceutically acceptable salt thereof, wherein Ar₁ is

A is

R₁ is —Cl, —Br, —I, —(C₁-C₆)alkyl, —NO₂, —CN, —OH, —OCH₃, —NH₂,—C(halo)₃, —CH(halo)₂, or —CH₂(halo); each R₂ is independently: (a)-halo, —CN, —OH, —O(C₁-C₆)alkyl, —NO₂, or —NH₂; (b) —(C₁-C₁₀)alkyl,—(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl,—(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,—(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, eachof which is unsubstituted or substituted with one or more R₅ groups; or(c) -phenyl, -naphthyl, —(C₁₄)aryl, or -(5- to 10-membered)heteroaryl,each of which is unsubstituted or substituted with one or more R₆groups; each R₃ is independently: (a) -halo, —CN, —OH, —O(C₁-C₆)alkyl,—NO₂, or —NH₂; (b) —(C₁-C₁₀)alkyl, —(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl,—(C₃-C₁₀)cycloalkyl, —(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl,—(C₅-C₁₀)cycloalkenyl, —(C₈-C₁₄)bicycloalkenyl,—(C₈-C₁₄)tricycloalkenyl, -(3- to 7-membered)heterocycle, or -(7- to10-membered)bicycloheterocycle, each of which is unsubstituted orsubstituted with one or more R₅ groups; or (c) -phenyl, -naphthyl,—(C₁₄)aryl or -(5- to 10-membered)heteroaryl, each of which isunsubstituted or substituted with one or more R₆ groups; R₄ is —H or—(C₁-C₆)alkyl; each R₅ is independently —CN, —OH, -halo, —N₃, —NO₂,—N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇,—SR₇, —S(O)R₇, or —S(O)₂R₇; each R₆ is independently —(C₁-C₆)alkyl,—(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,—(C₅-C₈)cycloalkenyl, -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃,—CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇,—NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or—S(O)₂R₇; each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—(C₃-C₅)heterocycle, —C(halo)₃, —CH₂(halo), or —CH(halo)₂; R₈ and R₉ areeach independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl,—(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃,—CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —N(R₇)₂, —CH═NR₇, —NR₇OH,—OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇;each -halo is —F, —Cl, —Br, or —I; n is an integer ranging from 0 to 3;m is 0 or 1; and x is 0 or
 1. 40. The compound of claim 39, wherein x is1 and A is —C(O)N(R₄)—.
 41. The compound of claim 39, wherein x is 1,and A is —C(S)N(R₄)—.
 42. The compound of claim 39, wherein n is
 0. 43.The compound of claim 39, wherein n is
 1. 44. The compound of claim 39,wherein x is
 0. 45. The compound of claim 39, wherein: R₁ is —CH₃, —CF₃,—Cl, —Br, or —I; m is 0; n is 0; x is 1; A is —C(O)—N(R₄)—; R₄ is —H; R₈is —H; and R₉ is —CH₃, —CF₃, —OCH₂CH₃, tert-butyl, —Cl, —Br, or —F. 46.The compound of claim 39, wherein: R₁ is —CH₃, —CF₃, —Cl, —Br, or —I; mis 1; R₃ is —(C₁-C₁₀)alkyl; n is 0; x is 1; A is —C(O)—N(R₄)—; R₄ is —H;R₈ is —H; and R₉ is —CH₃, —CF₃, —OCH₂CH₃, tert-butyl, —Cl, —Br, or —F.47. The compound of claim 46, wherein R₃ is —CH₃.
 48. The compound ofclaim 46, wherein the carbon to which R₃ is attached is in the (R)configuration.
 49. The compound of claim 46, wherein R₃ is attached to acarbon atom adjacent to a nitrogen atom attached to the—C(O)—N(R₁)-group.
 50. The compound of claim 39, wherein m is 1 and thecarbon to which R₃ is attached is in the (R) configuration.
 51. Acomposition comprising the compound or a pharmaceutically acceptablesalt of the compound of claim 1 and a pharmaceutically acceptablecarrier or excipient.
 52. A method for treating pain in an animal,comprising administering to an animal in need thereof an effectiveamount of the compound or a pharmaceutically acceptable salt of thecompound of claim
 1. 53. A method for preparing a composition comprisingthe step of admixing a compound or a pharmaceutically acceptable salt ofthe compound of claim 1 and a pharmaceutically acceptable carrier orexcipient.
 54. A compound selected from the group consisting of

and pharmaceutically acceptable salts thereof.
 55. A compound selectedfrom the group consisting of

and pharmaceutically acceptable salts thereof.
 56. A compound selectedfrom the group consisting of

and pharmaceutically acceptable salts thereof.
 57. A compound offormula:

or a pharmaceutically acceptable salt thereof, wherein Ar₁ is

Ar₂ is

R₁ is -halo, —(C₁-C₆)alkyl, —NO₂, —CN, —OH, —OCH₃, —NH₂, —C(halo)₃,—CH(halo)₂, or —CH₂(halo); each R₂ is independently: (a) -halo, —CN,—OH, —O(C₁-C₆)alkyl, —NO₂, or —NH₂; (b) —(C₁-C₁₀)alkyl,—(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl,—(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,—(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, eachof which is unsubstituted or substituted with one or more R₅ groups; or(c) -phenyl, -naphthyl, —(C₁₄)aryl, or -(5- to 10-membered)heteroaryl,each of which is unsubstituted or substituted with one or more R₆groups; R₃ is —H or —CH₃; each R₅ is independently —CN, —OH, -halo, —N₃,—NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇,—OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇; each R₆ is independently—(C₁-C₆)alkyl, —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,—(C₅-C₈)cycloalkenyl, -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃,—CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇,—NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or—S(O)₂R₇; each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—(C₃-C₅)heterocycle, —C(halo)₃, —CH₂(halo), or —CH(halo)₂; R₈ and R₉ areeach independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl,—(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃,—CH(halo)₂, —CH₂(halo), —OC(halo)₃, —OCH(halo)₂, —OCH₂(halo), —CN, —OH,-halo, —N₃, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇,—OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇, each -halo is —F, —Cl, —Br, or—I; and n is an integer ranging from 0 to
 3. 58. A compound of formula:

or a pharmaceutically acceptable salt thereof, wherein Ar₁ is

A is

R₁ is -halo, —(C₁-C₆)alkyl, —NO₂, —CN, —OH, —OCH₃, —NH₂, —C(halo)₃,—CH(halo)₂, or —CH₂(halo); each R₂ is independently: (a) -halo, —CN,—OH, —O(C₁-C₆)alkyl, —NO₂, or —NH₂; (b) —(C₁-C₁₀)alkyl,—(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —C₃-C₁₀)cycloalkyl,—(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,—(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to7-membered)heteroeycle, or -(7- to 10-membered)bicycloheterocycle, eachof which is unsubstituted or substituted with one or more R₅ groups; or(c) -phenyl, -naphthyl, —(C₁₄)aryl, or -(5- 10-membered)heteroaryl, eachof which is unsubstituted or substituted with one or more R₆ groups; R₃is —CH₃; R₄ is —H or —(C₁-C₆)alkyl; each R₅ is independently —CN, —OH,-halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇,—OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇; each R₆ isindependently —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl,—(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, —(C₃-C₅)heterocycle,—C(halo)₃, —CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R7)₂,—CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇,—S(O)R₇, or —S(O)R₇; each R₇ is independently —H, —(C₁-C₆)alkyl,—(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,—(C₅-C₈)cycloalkenyl, -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃,—CH₂(halo), or —OH(halo)₂; R₈ and R₉ are each independently —H,—(C₁-C₆)alkyl, —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,—(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃, —CH(halo)₂, —CH₂(halo),—OC(halo)₃, —OCH(halo)₂, —OCH₂(halo), —CN, —OH, -halo, —N₃, —N(R₇)₂,—CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇,—S(O)R₇, or —S(O)R₇; each -halo is —F, —Cl, —Br, or —I; n is an integerranging from 0 to 3; x is 0 or 1; when x is 0, Ar₂ is

and when x is 1, Ar₂ is


59. A composition comprising: (i) an effective amount of a compound offormula:

or a pharmaceutically acceptable salt thereof, wherein Ar₁ is

Ar₂ is

R₁ is -halo, —(C₁-C₆)alkyl, —NO₂, —CN, —OH, —OCH₃, —NH₂, —C(halo)₃,—CH(halo)₂, or —CH₂(halo); each R₂ is independently: (a) -halo, —CN,—OH, —O(C₁-C₆)alkyl, —NO₂, or —NH₂; (b) —(C₁-C₁₀)alkyl,—(C₂-C₁₀)alkenyl, —(C₂-C₁₀)alkynyl, —(C₃-C₁₀)cycloalkyl,—(C₈-C₁₄)bicycloalkyl, —(C₈-C₁₄)tricycloalkyl, —(C₅-C₁₀)cycloalkenyl,—(C₈-C₁₄)bicycloalkenyl, —(C₈-C₁₄)tricycloalkenyl, -(3- to7-membered)heterocycle, or -(7- to 10-membered)bicycloheterocycle, eachof which is unsubstituted or substituted with one or more R₅ groups; or(c) -phenyl, -naphthyl, —(C₁₄)aryl, or -(5- to 10-membered)heteroaryl,each of which is unsubstituted or substituted with one or more R₆groups; R₃ is —H or —CH₃: each R₅ is independently —CN, —OH, -halo, —N₃,—NO₂, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇,—OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇; each R₆ is independently—(C₁-C₆)alkyl, —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl,—(C₅-C₈)cycloalkenyl, -phenyl, —(C₃-C₅)heterocycle, —C(halo)₃,—CH(halo)₂, —CH₂(halo), —CN, —OH, -halo, —N₃, —NO₂, —N(R₇)₂, —CH═NR₇,—NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇, —OC(O)OR₇, —SR₇, —S(O)R₇, or—S(O)₂R₇; each R₇ is independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl,—(C₂-C₆)alkynyl, —(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl,—(C₃-C₅)heterocycle, —C(halo)₃, —CH₂(halo), or —CH(halo)₂; R₈ and R₉ areeach independently —H, —(C₁-C₆)alkyl, —(C₂-C₆)alkenyl, —(C₂-C₆)alkynyl,—(C₃-C₈)cycloalkyl, —(C₅-C₈)cycloalkenyl, -phenyl, —C(halo)₃,—CH(halo)₂, —CH₂(halo), —OC(halo)₃, —OCH(halo)₂, —OCH₂(halo), —CN, —OH,-halo, —N₃, —N(R₇)₂, —CH═NR₇, —NR₇OH, —OR₇, —COR₇, —C(O)OR₇, —OC(O)R₇,—OC(O)OR₇, —SR₇, —S(O)R₇, or —S(O)₂R₇; each -halo is —F, —Cl, —Br, or—I; and n is an integer ranging from 0 to 3; and (ii) a pharmaceuticallyacceptable carrier or excipient.
 60. A compound selected from the groupconsisting of

and pharmaceutically acceptable salts thereof.
 61. The compound of claim1, wherein: R₁ is —CH₃, —CF₃, —Cl, —Br, or —I; m is 0; n is 0; x is 1; Ais —C(S)—N(R₄)—; R₄ is —H; R₈ is —H; and R₉ is —CH₃, —CF₃, —OCH₂CH₃,tert-butyl, —Cl, —Br, or —F.
 62. The compound of claim 61, wherein R₁ is—CH₃ and R₉ is —Cl.
 63. The compound of claim 61, wherein R₁ is —CH₃ andR₉ is —Br.
 64. The compound of claim 61, wherein R₁ is —CH₃ and R₉ is—F.
 65. The compound of claim 61, wherein R₁ is —Cl and R₉ is —Cl. 66.The compound of claim 61, wherein R₁ is —Cl and R₉ is —Br.
 67. Thecompound of claim 61, wherein R₁ is —Cl and R₉ is —F.
 68. The compoundof claim 1, wherein: R₁ is —CH₃, —CF₃, —Cl, —Br, or —I; m is 1; R₃ is—(C₁-C₁₀)alkyl; n is 0; x is 1; A is —C(S)—N(R₁)—; R₄ is —H; R₈ is —H;and R₉ is —CH₃, —CF₃, —OCH₂CH₃, tert-butyl, —Cl, —Br, or —F.
 69. Thecompound of claim 68, wherein R₃ is —CH₃.
 70. The compound of claim 68,wherein the carbon to which R₃ is attached is in the (R) configuration.71. The compound of claim 68, wherein R₃ is attached to a carbon atomadjacent to a nitrogen atom attached to the —C(S)—N(R₄-group.
 72. Thecompound of claim 68, wherein R₁ is —CH₃ and R₉ is —Cl.
 73. The compoundof claim 72, wherein the carbon to which R₃ is attached is in the (R)configuration.
 74. The compound of claim 68, wherein R₁ is —CH₃ and R₉is —Br.
 75. The compound of claim 74, wherein the carbon to which R₃ isattached is in the (R) configuration.
 76. The compound of claim 68,wherein R₁ is —CH₃ and R₉ is —F.
 77. The compound of claim 76, whereinthe carbon to which R₃ is attached is in the (R) configuration.
 78. Thecompound of claim 68, wherein R₁ is —Cl and R₉ is —Cl.
 79. The compoundof claim 78, wherein the carbon to which R₃ is attached is in the (R)configuration.
 80. The compound of claim 68, wherein R₁ is —Cl and R₉ is—Br.
 81. The compound of claim 80, wherein the carbon to which R₃ isattached is in the (R) configuration.
 82. The compound of claim 68,wherein R₁ is —Cl and R₉ is —F.
 83. The compound of claim 82, whereinthe carbon to which R₃ is attached is in the (R) configuration.
 84. Thecompound of claim 45, wherein R₁ is —CH₃ and R₉ is —Cl.
 85. The compoundof claim 45, wherein R₁ is —CH₃ and R₉ is —Br.
 86. The compound of claim45, wherein R₁ is —CH₃ and R₉ is —F.
 87. The compound of claim 45,wherein R₁ is —Cl and R₉ is —Cl.
 88. The compound of claim 45, whereinR₁ is —Cl and R₉ is —Br.
 89. The compound of claim 45, wherein R₁ is —Cland R₉ is —F.
 90. The compound of claim 46, wherein R₁ is —CH₃ and R₉ is—Cl.
 91. The compound of claim 90, wherein the carbon to which R₃ isattached is in the (R) configuration.
 92. The compound of claim 46,wherein R₁ is —CH₃ and R₉ is —Br.
 93. The compound of claim 92, whereinthe carbon to which R₃ is attached is in the (R) configuration.
 94. Thecompound of claim 46, wherein R₁ is —CH₃ and R₉ is —F.
 95. The compoundof claim 94, wherein the carbon to which R₃ is attached is in the (R)configuration.
 96. The compound of claim 46, wherein R₁ is —Cl and R₉ is—Cl.
 97. The compound of claim 96, wherein the carbon to which R₃ isattached is in the (R) configuration.
 98. The compound of claim 46,wherein R₁ is —Cl and R₉ is —Br.
 99. The compound of claim 98, whereinthe carbon to which R₃ is attached is in the (R) configuration.
 100. Thecompound of claim 46, wherein R₁ is —Cl and R₉ is —F.
 101. The compoundof claim 100, wherein the carbon to which R₃ is attached is in the (R)configuration.
 102. The compound of claim 39, wherein: R₁ is —CH₃, —CF₃,—Cl, —Br, or —I; m is 0; n is 0; x is 1; A is —C(S)—N(R₄)—; R₄ is —H; R₅is —H; and R₉ is —CH₃, —CF₃, —OCH₂OH₃, tert-butyl, —Cl, —Br, or —F. 103.The compound of claim 102, wherein R₁ is —CH₃ and R₉ is —Cl.
 104. Thecompound of claim 102, wherein R₁ is —CH₃ and R₉ is —Br.
 105. Thecompound of claim 102, wherein R₁ is —CH₃ and R₉ is —F.
 106. Thecompound of claim 102, wherein R₁ is —Cl and R₉ is —Cl.
 107. Thecompound of claim 102, wherein R₁ is —Cl and R₉ is —Br.
 108. Thecompound of claim 102, wherein R₁ is —Cl and R₉ is —F.
 109. The compoundof claim 39, wherein: R₁ is —CH₃, —CF₃, —Cl, —Br, or —I; m is 1; R₃ is—(C₁-C₁₀)alkyl; n is 0; x is 1; A is —C(S)—N(R₄)—; R₄ is —H; R₈ is —H;and R₉ is —CH₃, —CF₃, —OCH₂CH₃, tert-butyl, —Cl, —Br, or —F.
 110. Thecompound of claim 109, wherein R₃ is —CH₃.
 111. The compound of claim109, wherein the carbon to which R₃ is attached is in the (R)configuration.
 112. The compound of claim 109, wherein R₃ is attached toa carbon atom adjacent to a nitrogen atom attached to the—C(S)—N(R₄)-group.
 113. The compound of claim 109, wherein R₁ is —CH₃and R₉ is —Cl.
 114. The compound of claim 113, wherein the carbon towhich R₃ is attached is in the (R) configuration.
 115. The compound ofclaim 109, wherein R₁ is —CH₃ and R₉ is —Br.
 116. The compound of claim115, wherein the carbon to which R₃ is attached is in the (R)configuration.
 117. The compound of claim 109, wherein R₁ is —CH₃ and R₉is —F.
 118. The compound of claim 117, wherein the carbon to which R₃ isattached is in the (R) configuration.
 119. The compound of claim 109,wherein R₁ is —Cl and R₉ is —Cl.
 120. The compound of claim 119, whereinthe carbon to which R₃ is attached is in the (R) configuration.
 121. Thecompound of claim 109, wherein R₁ is —Cl and R₉ is —Br.
 122. Thecompound of claim 121, wherein the carbon to which R₃ is attached is inthe (R) configuration.
 123. The compound of claim 109, wherein R₁ is —Cland R₉ is —F.
 124. The compound of claim 123, wherein the carbon towhich R₃ is attached is in the (R) configuration.
 125. A compositioncomprising the compound or a pharmaceutically acceptable salt of thecompound of claim 13 and a pharmaceutically acceptable carrier orexcipient.
 126. A composition comprising the compound or apharmaceutically acceptable salt of the compound of claim 31 and apharmaceutically acceptable carrier or excipient.
 127. A compositioncomprising the compound or a pharmaceutically acceptable salt of thecompound of claim 39 and a pharmaceutically acceptable carrier orexcipient.
 128. A composition comprising the compound or apharmaceutically acceptable salt of the compound of claim 54 and apharmaceutically acceptable carrier or excipient.
 129. A compositioncomprising the compound or a pharmaceutically acceptable salt of thecompound of claim 55 and a pharmaceutically acceptable carrier orexcipient.
 130. A composition comprising the compound or apharmaceutically acceptable salt of the compound of claim 56 and apharmaceutically acceptable carrier or excipient.
 131. A compositioncomprising the compound or a pharmaceutically acceptable salt of thecompound of claim 57 and a pharmaceutically acceptable carrier orexcipient.
 132. A composition comprising the compound or apharmaceutically acceptable salt of the compound of claim 58 and apharmaceutically acceptable carrier or excipient.
 133. A compositioncomprising the compound or a pharmaceutically acceptable salt of thecompound of claim 60 and a pharmaceutically acceptable carrier orexcipient.
 134. A method for preparing a composition comprising the stepof admixing a compound or a pharmaceutically acceptable salt of thecompound of claim 13 and a pharmaceutically acceptable carrier orexcipient.
 135. A method for preparing a composition comprising the stepof admixing a compound or a pharmaceutically acceptable salt of thecompound of claim 31 and a pharmaceutically acceptable carrier orexcipient.
 136. A method for preparing a composition comprising the stepof admixing a compound or a pharmaceutically acceptable salt of thecompound of claim 39 and a pharmaceutically acceptable carrier orexcipient.
 137. A method for preparing a composition comprising the stepof admixing a compound or a pharmaceutically acceptable salt of thecompound of claim 54 and a pharmaceutically acceptable carrier orexcipient.
 138. A method for preparing a composition comprising the stepof admixing a compound or a pharmaceutically acceptable salt of thecompound of claim 55 and a pharmaceutically acceptable carrier orexcipient.
 139. A method for preparing a composition comprising the stepof admixing a compound or a pharmaceutically acceptable salt of thecompound of claim 56 and a pharmaceutically acceptable carrier orexcipient.
 140. A method for preparing a composition comprising the stepof admixing a compound or a pharmaceutically acceptable salt of thecompound of claim 57 and a pharmaceutically acceptable carrier orexcipient.
 141. A method for preparing a composition comprising the stepof admixing a compound or a pharmaceutically acceptable salt of thecompound of claim 58 and a pharmaceutically acceptable carrier orexcipient.
 142. A method for preparing the composition of claim 59comprising the step of admixing the compound or the pharmaceuticallyacceptable salt of the compound of formula (V) and the pharmaceuticallyacceptable carrier or excipient.
 143. A method for preparing acomposition comprising the step of admixing a compound or apharmaceutically acceptable salt of the compound of claim 60 and apharmaceutically acceptable carrier or excipient.
 144. The compound ofclaim 31 selected from the group consisting of

and pharmaceutically acceptable salts thereof.